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Inhibitors Agonists Screening LibrarieswwwMedChemExpresscom

JAKSTAT Signaling

The Janus kinase (JAK)signal transducer and activator of transcription (STAT) pathway is central to signaling by cytokinereceptors a superfamily of more than 30 transmembrane proteins that recognize specific cytokines and is critical in bloodformation and immune response Canonical JAKSTAT signaling begins with the association of cytokines and theircorresponding transmembrane receptors Activated JAKs then phosphorylate latent STAT monomers leading todimerization nuclear translocation and DNA binding In mammals there are four JAKs (JAK1 JAK2 JAK3 TYK2) and sevenSTATs (STAT1 STAT2 STAT3 STAT4 STAT5a STAT5b STAT6)JAKs are an integral component of the receptor subunit with very little release or exchange into the cytoplasm and assuch are located primarily at the plasma membrane STAT has seven conserved features an N-terminal domain (NT) acoiled-coil domain (CC) a central DNA-binding domain (DBD) a linker region an SH2 domain followed by a singleconserved tyrosine residue and a C-terminal transactivation domain (TAD) JAK phosphorylation of the STAT proteinsthen results in a spatial reorganisation of the dimer complex and translocates to the nucleus Once in the nucleus STATdimmers are stabilised by NTNT interactions and bind cooperatively to tandem sequence elements within promoterregions to activate the transcription of specific gene subsetsAberrant activation of the JAKSTAT pathway has been reported in a variety of diseases including inflammatoryconditions hematologic malignancies and solid tumors More recently human myeloproliferative neoplasms arediscovered to be associated with a unique acquired somatic mutation in JAK2 (JAK2 V617F) rare exon 12 JAK2 mutationsor thrombopoietin receptor mutations that constitutively activate wild-type JAK2 As a result several drug companieshave begun to develop therapeutics that inhibit the function of JAK tyrosine kinases Currently several JAK-targetingdrugs have been used in the clinic for treating diseases including rheumatoid arthritis and myeloproliferative References[1] Kiu H et al Growth Factors 2012 Apr30(2)88-106[2] Quintaacutes-Cardama A et al Clin Cancer Res 2013 Apr 1519(8)1933-40[3] Villarino AV et al J Immunol 2015 Jan 1194(1)21-7

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bull EGFR 3

bull JAK 15

bull Pim 23

bull STAT 26

Inhibitors Agonists Screening LibrarieswwwMedChemExpresscom

Target List in JAKSTAT Signaling

wwwMedChemExpresscom 3

bull EGFR 3

bull JAK 15

bull Pim 23

bull STAT 26

Inhibitors Agonists Screening LibrarieswwwMedChemExpresscom

Target List in JAKSTAT Signaling

EGFREpidermal growth factor receptorErbB-1HER1

The EGFR family of receptor tyrosine kinases (RTK) comprises fourdistinct receptors the EGFR (also known as ErbB-1HER1) ErbB-2(neu HER2) ErbB-3 (HER3) and ErbB-4 (HER4) All EGFR familymembers are characterized by a modular structure consisting of anextracellular ligand-binding domain a single hydrophobictransmembrane region and the intracellular part harbouring thehighly conserved tyrosine kinase domain The ErbB family of receptortyrosine kinases (RTKs) couples binding of extracellular growth factorligands to intracellular signaling pathways regulating diverse biologicresponses including proliferation differentiation cell motility andsurvival Ten growth factors and their ErbB specificities are EGF

amphiregulin (AR) and TGF bind ErbB-1 betacellulin heparin binding EGF-like growth factor and epiregulin bindboth ErbB-1 and ErbB-4 the neuregulins (also called heregulins and Neu differentiation factors) NRG-1 and NRG-2bind ErbB-3 and ErbB-4 and NRG-3 and NRG-4 bind ErbB-4 No known ligand binds ErbB-2 The three bestcharacterized signaling pathways induced through ErbBs are Rasndashmitogen-activated protein kinase (Ras-MAPK)phosphatidylinositol 3_ kinase-protein kinase B (PI3K-PKBAkt) and phospholipase Cndashprotein kinase C (PLC-PKC)pathways

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Purity 9999Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9642Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9885Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity 9984Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity 9974Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9931Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity 9991Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

EGFR Inhibitors amp Modulators

Bioactivity AEE788 is an inhibitor of the and with EGFR ErbB2 IC50values of 2 and 6 nM respectively

Bioactivity Afatinib (BIBW 2992) is an irreversible family inhibitorEGFRwith s of 05 nM 04 nM 10 nM and 14 nM for EGFR IC50

wt

EGFR EGFR and HER2 respectivelyL858R L858RT790M

Bioactivity Afatinib dimaleate is an irreversible family inhibitorEGFRwith s of 05 nM 04 nM 10 nM and 14 nM for EGFR IC50

wt

EGFR EGFR and HER2 respectivelyL858R L858RT790M

Bioactivity AG 555 is an tyrosine kinase inhibitorEGFR

Bioactivity AG-1478 is a selective tyrosine kinase inhibitor withEGFR of 3 nMIC50

Bioactivity AG-490 is a tyrosine kinase inhibitor that inhibits EGFR and Stat-3 JAK23

Bioactivity Allitinib (AST1306) is a selective irreversible andEGFR inhibitor with s of 05 and 3 nM respectivelyErbB2 IC50

Bioactivity Allitinib tosylate (AST-1306 TsOH) is a novel irreversibleinhibitor of EGFR and ErbB2 with IC50 of 05 nM and 3 nM alsoeffective in mutation EGFR T790ML858R more potent toErbB2-overexpressing cells 3000-fold selective for ErbBfamily than other kinases IC50 value 053 nM (EGFRErb2)[1]hellip

Bioactivity The product is the analog of ARRY-380 ARRY-380 is a potentand selective HER2 inhibitor with IC50 of 8 nM equipotentagainst truncated p95-HER2 500-fold more selective for HER2versus EGFR

Bioactivity AST2818 mesylate is an inhibitorEGFR

AEE788 (NVP-AEE 788) Cat No HY-10045

Afatinib (BIBW 2992) Cat No HY-10261

Afatinib dimaleate (BIBW 2992MA2 BIBW2992 Afatinib) Cat No HY-10261A

AG 555 (Tyrphostin AG 555) Cat No HY-15336

AG-1478 (Tyrphostin AG-1478 NSC 693255) Cat No HY-13524

AG-490 (Tyrphostin AG 490) Cat No HY-12000

Allitinib (AST-1306 ALS 1306) Cat No HY-15375

Allitinib tosylate (AST-1306 (TsOH)) Cat No HY-13427

ARRY-380 analog Cat No HY-10531

AST2818 mesylate Cat No HY-112870A

Purity 9937Clinical Data Phase 2Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9982Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 1Size 10 mg 50 mg

Purity gt98Clinical Data Phase 1Size 1 mg 5 mg 10 mg 20 mg

Purity 9949Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9849Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9926Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Bioactivity Astragaloside VI could activate signalling pathwayEGFRERKto improve wound healing

Bioactivity AV-412 (MP412) is an inhibitor with s of 075 05EGFR IC50

079 23 19 nM for EGFR EGFR EGFR EGFRL858R T790M

and ErbB2 respectivelyL858RT790M

Bioactivity AV-412 (MP412) is an inhibitor with s of 075 05EGFR IC50

079 23 19 nM for EGFR EGFR EGFR EGFRL858R T790M

and ErbB2 respectivelyL858RT790M

Bioactivity Avitinib maleate is a pyrrolopyrimidine-based irreversibleepidermal growth factor receptor ( ) inhibitor with anEGFR

of 768 nMIC50

Bioactivity AZ-5104 is an active demethylated metabolite of AZD 9291AZ-5104 is an inhibitor with s of 1 6 1 25 and 7EGFR IC50

nM for EGFR EGFR EGFR EGFR andL858RT790M L858R L861Q

ErbB4 respectively

Bioactivity AZD3759 is a potent oral active central nervoussystem-penetrant inhibitor At K ATPEGFR mconcentrations the s are 03 02 and 02 nM for EGFRIC50

EGFR and EGFR respectivelywt L858R exon 19Del

Bioactivity BGB-102 is a potent multi-kinase inhibitor against EGFR and with s of 96 nM 18 nM and 403 nMHER2 HER4 IC50

respectively

Bioactivity AC480 (BMS-599626) is a selective and efficacious inhibitor ofHER1 and HER2 with IC50 of 20 nM and 30 nM ~8-fold lesspotent to HER4 gt100-fold to VEGFR2 c-Kit Lck MET etcIC50 value 20 nM (HER1) 30 nM (HER2) [1] Target HER1HER2in vitro BMS-599626 inhibited HER1 and HER2 with IC50 of 20hellip

Bioactivity AC480 (BMS-599626) is a selective and efficacious inhibitor ofHER1 and HER2 with IC50 of 20 nM and 30 nM ~8-fold lesspotent to HER4 gt100-fold to VEGFR2 c-Kit Lck MET etc

Bioactivity BMS-690514 is a potent and orally active inhibitor of EGFRand has s of 5 20 and 60 nM for EGFR HER 2 andVEGFR IC50HER 4 respectively

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Astragaloside VI Cat No HY-N6577

AV-412 (MP412) Cat No HY-10346

AV-412 free base (MP-412 free base) Cat No HY-10346A

Avitinib maleate Cat No HY-19816A

AZ-5104 Cat No HY-B0793

AZD3759 Cat No HY-18750

BGB-102 (JNJ-26483327) Cat No HY-15732

BMS-599626 (AC480) Cat No HY-10251

BMS-599626 Hydrochloride (AC480) Cat No HY-12010

BMS-690514 Cat No HY-10333

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Purity 9983Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9959Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9962Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9806Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9706Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9963Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 9970Clinical Data LaunchedSize 1 mg 5 mg

Purity 9851Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity 9910Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity 9989Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Bioactivity Butein a plant polyphenol isolated from Rhus vernicifluainhibit the activation of protein tyrosine kinase and EGFRtarget EGFR [1] In vitro 1) Butein inhibited the activationof AKT extracellular signal-regulated kinase (ERKs) and p38kinases in the presence of cisplatin[2] 2) FoxO3a and itshellip

Bioactivity Canertinib (CI-1033PD-183805) is a potent and irreversible inhibitor inhibits cellular and EGFR EGFR ErbB2

autophosphorylation with s of 74 and 9 nMIC50

Bioactivity Canertinib dihydrochloride (CI-1033PD-183805) is a potent andirreversible inhibitor inhibits cellular andEGFR EGFR

autophosphorylation with s of 74 and 9 nMErbB2 IC50

Bioactivity Cetuximab is a monoclonal antibody that inhibits epidermalgrowth factor receptor ( ) with a of 0201 nM forEGFR Kdsoluble EGFR by SPR Cetuximab has potent antitumor activity

Bioactivity Chrysophanol (Chrysophanic acid) is a natural anthraquinonewhich inhibits EGF-induced phosphorylation of andEGFRsuppresses activation of and AKT mTOR p70S6K

Bioactivity CL-387785(EKI785 WAY-EKI 785) is an irreversible inhibitor ofEGFR with IC50 of 370+-120 pM is able to overcome resistancecaused by the T790M mutation on a functional level

Bioactivity CNX-2006 is a mutant-selective and irreversible EGFRinhibitor with an below 20 nM for EGFR IC50

T790MBioactivity CP-724714 is a potent selective inhibitor of HER2ErbB2 with

IC50 of 10 nM gt640-fold selectivity against EGFR InsRIRG-1R PDGFR VEGFR2 Abl Src c-Met etc Phase 2

Bioactivity CUDC-101 is a potent inhibitor of and withHDAC EGFR HER2s of 44 24 and 157 nM respectivelyIC50

Bioactivity Dacomitinib is a specific and irreversible inhibitor of the family of kinases with s of 6 nM 457 nM and 737ERBB IC50

nM for and respectivelyEGFR ERBB2 ERBB4

Butein (2rsquo344rsquo-tetrahydroxy Chalcone) Cat No HY-16558

Canertinib (CI-1033 PD-183805) Cat No HY-10367

Canertinib dihydrochloride (Canertinib CI-1033

dihydrochloride PD-183805 dihydrochloride) Cat No HY-10367A

Cetuximab (C225) Cat No HY-P9905

Chrysophanol (Chrysophanic acid) Cat No HY-13595

CL-387785 (EKI-785 WAY-EKI 785) Cat No HY-10325

CNX-2006 Cat No HY-13897

CP-724714 Cat No HY-14674

CUDC-101 Cat No HY-10223

Dacomitinib (PF-00299804 PF-299804) Cat No HY-13272

Purity 9692Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data LaunchedSize 100 mg 500 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9933Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9890Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Bioactivity Daphnetin (78-dihydroxycoumarin) one coumarin derivativeisolated from plants of the is a Genus Daphne protein kinaseinhibitor with of 767 μM 933 μM and 2501 μM forIC s50

EGFR PKA and PKC respectively Daphnehellipin vitro [1] [2]

Bioactivity Desmethyl Erlotinib (OSI-420) is an active metabolite oferlotinib which is a potent EGFR tyrosin kinase inhibitor

Bioactivity EAI045 is an allosteric inhibitor of mutant with sEGFR IC50

of 19 0019 019 and 0002 μM for EGFR EGFR EGFRL858R

and EGFR at 10 μM ATP respectivelyT790M L858RT790M

Bioactivity EGFR-IN-2 is a a noncovalent irreversible mutant-selectivesecond generation inhibitorEGFR

Bioactivity EGFR-IN-3 is an epidermal growth factor receptor (EGFR)inhibitor

Bioactivity Epertinib is a potent oral reversible and selectivetyrosine kinase inhibitor of and withEGFR HER2 HER4

s of 148 nM 715 nM and 249 nM respectively EpertinibIC50shows potent antitumor activity

Bioactivity Erlotinib is a medication for the treatment of non-small celllung cancer It inhibits purified kinase with an ofEGFR IC502 nM

Bioactivity Erlotinib hydrochloride inhibits purified kinase with anEGFR of 2 nMIC50

Bioactivity Erlotinib mesylate inhibits purified kinase with an EGFR IC50of 2 nM

Bioactivity Falnidamol (BIBX 1382) is a potent selective inhibitor ofEGFR tyrosine kinase (IC = 3 nM) displays gt 1000-fold50lower potency against ErbB2 (IC = 34 μM) and a range of50other related tyrosine kinases (IC gt 10 μM)50

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Daphnetin (78-Dihydroxycoumarin) Cat No HY-N0281

Desmethyl Erlotinib (OSI-420 CP-473420) Cat No HY-13256

EAI045 Cat No HY-100213

EGFR-IN-2 Cat No HY-100520

EGFR-IN-3 Cat No HY-19815

Epertinib (S-22611) Cat No HY-107367

Erlotinib (NSC 718781 OSI-744 R1415) Cat No HY-50896

Erlotinib Hydrochloride (CP-358774 OSI-774 NSC 718781) Cat No HY-12008

Erlotinib mesylate (CP-358774 OSI-774 NSC 718781 R 1415) Cat No HY-12008A

Falnidamol (BIBX 1382) Cat No HY-10322

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Purity 9800Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9858Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 500 mg 1 g

Purity 9983Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 500 mg 1 g

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9980Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9964Clinical Data Phase 4Size 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9933Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 500 mg 1 g 5 g

Purity 9989Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg 1 g 5 g

Purity 9824Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Bioactivity FIIN-3 is an irreversible inhibitor of with an ofFGFR IC50131 21 314 and 353 nM for FGFR1 FGFR2 FGFR3 and FGFR4respectively

Bioactivity Gefitinib (ZD1839) is a inhibitor withEGFR tyrosine kinase of 2-37 nM in NR6wtEGFR cellsIC50

Bioactivity Gefitinib hydrochloride is an inhibitor that specificallybinds and inhibits the with the EGFR tyrosine kinase IC50value of 2-37 nM in NR6wtEGFR cells

Bioactivity Genistein a soy isoflavone is a multiple tyrosine kinasesinhibitor which acts as a chemotherapeutic agent againstdifferent types of cancer mainly by altering apoptosis thecell cycle and angiogenesis and inhibiting metastasis

Bioactivity HS-10296 hydrochloride is an orally available andthird-Generation inhibitor of epidermal growth factor receptor

-activating mutations and -resistant mutation(EGFR) T790Mwith limited activity against wild-type EGFR

Bioactivity Icotinib (BPI-2009) is a potent and specific inhibitorEGFRwith an of 5 nM also inhibits mutant EGFR EGFRIC50

L858R

EGFR and EGFR L858RT790M T790M L861Q

Bioactivity Icotinib Hydrochloride (BPI-2009) is a potent and specific inhibitor with an of 5 nM also inhibits mutantEGFR IC50

EGFR EGFR EGFR and EGFRL858R L858RT790M T790M

L861Q

Bioactivity Lapatinib (GW572016) is a potent and inhibitorEGFR ErbB2with s of 102 and 98 nM respectivelyIC50

Bioactivity Lapatinib ditosylate is a potent and inhibitorEGFR ErbB2with of 102 and 98 nM respectivelyIC50

Bioactivity Lazertinib is a potent highly mutant-selective blood-brainbarrier permeable orally available and irreversiblethird-generation tyrosine kinase inhibitor and can beEGFRused in the research of non-small cell lung cancer

FIIN-3 Cat No HY-18603

Gefitinib (ZD1839) Cat No HY-50895

Gefitinib hydrochloride (ZD-1839 hydrochloride) Cat No HY-50895A

Genistein (NPI 031L) Cat No HY-14596

HS-10296 hydrochloride Cat No HY-112823B

Icotinib (BPI-2009) Cat No HY-15164A

Icotinib Hydrochloride (BPI-2009H) Cat No HY-15164

Lapatinib (GW572016) Cat No HY-50898

Lapatinib ditosylate (GW-572016 ditosylate) Cat No HY-50898A

Lazertinib (YH25448 GNS-1480) Cat No HY-109061

Purity 9884Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg

Purity 9957Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9859Clinical Data Phase 3Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity gt98Clinical Data Phase 3Size 1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9988Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9894Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9991Clinical Data Phase 1Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9865Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9800Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity BGB-283 is a novel and potent Kinase and inhibitorRaf EGFRwith values of 23 and 29 nM for recombinant BRaf IC50

V600E

and EGFR respectively

Bioactivity MTX-211 is a dual inhibitor of and used for theEGFR PI3Ktreatment of cancer and other diseases

Bioactivity Mubritinib (TAK-165) is a potent and selective EGFR2HER2inhibitor with an of 6 nMIC50

Bioactivity Mutant EGFR inhibitor is a potent and selective mutant EGFRinhibitor extracted from patent WO 2013014448 A1 inhibitsEGFR EGFR and EGFR L858R Exon 19 deletion T790M

Bioactivity Mutated EGFR-IN-1 is a useful intermediate for the inhibitorsdesign for mutated EGFR such as L858R EGFR Exonl9 deletionactivating mutant and T790M resistance mutant IC50 valueTarget Mutated EGFR inhibitor More information can be foundin Patent WO 2013014448 A12 - (2 4 5 - substitutedhellip

Bioactivity Naquotinib (ASP8273) is an orally available mutant-selectiveand irreversible inhibitor with s of 8-33 nM towardEGFR IC50EGFR mutants and 230 nM for EGFR

Bioactivity Naquotinib mesylate (ASP8273) is an orally availablemutant-selective and irreversible inhibitor with sEGFR IC50of 8-33 nM toward EGFR mutants and 230 nM for EGFR

Bioactivity Nazartinib (EGF816) is a novel covalent mutant-selective inhibitor with and of 31 nM and 0222 min EGFR Ki Kinact

minus1

on EGFR(L858R790M) mutant respectively

Bioactivity Nazartinib mesylate (EGF816 mesylate) is a novel covalentmutant-selective inhibitor with and of 31 nMEGFR Ki Kinact

and 0222 min on EGFR(L858R790M) mutant respectivelyminus1

Bioactivity Neratinib is an orally available irreversible tyrosine kinaseinhibitor with s of 59 nM and 92 nM for HER2 and EGFRIC50respectively

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Lifirafenib (BGB-283) Cat No HY-18957

MTX-211 Cat No HY-107364

Mubritinib (TAK-165) Cat No HY-13501

Mutant EGFR inhibitor Cat No HY-13984

Mutated EGFR-IN-1 Cat No HY-78869

Naquotinib (ASP8273) Cat No HY-19729

Naquotinib mesylate (ASP8273) Cat No HY-19803

Nazartinib (EGF816) Cat No HY-12872

Nazartinib mesylate (EGF816 (mesylate)) Cat No HY-12872A

Neratinib (HKI-272) Cat No HY-32721

wwwMedChemExpresscom 11

Purity 9818Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9828Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9862Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9994Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9996Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9995Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg 1 g

Purity 9995Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9840Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Bioactivity NRC-2694 is an epidermal growth factor receptor ( )EGFRantagonist with anti-cancer and anti-proliferative properties

Bioactivity Olmutinib (HM61713 BI-1482694) is an irreversible EGFRtyrosine kinase inhibitor that binds to a cysteine residuenear the kinase domain

Bioactivity Osimertinib (AZD-9291) is an irreversible and mutant selective inhibitor with s of 12 and 1 nM against EGFR EGFR IC50

L858R

and EGFR respectivelyL858RT790M

Bioactivity Osimertinib dimesylate (AZD-9291 dimesylate) is anirreversible and mutant selective inhibitor with sEGFR IC50

of 12 and 1 nM against EGFR and EGFR L858R L858RT790M

respectively

Bioactivity Osimertinib mesylate (AZD-9291 mesylate) is an irreversibleand mutant selective inhibitor with s of 12 and 1 nMEGFR IC50

against EGFR and EGFR respectivelyL858R L858RT790M

Bioactivity PD153035 (SU 5271) is a potent inhibitor with andEGFR Ki of 6 and 25 pM respectivelyIC50

Bioactivity PD153035 (ZM 252868 AG 1517 SU 5271) is a potent EGFRinhibitor with and of 6 and 25 pM respectivelyKi IC50

Bioactivity PD158780 is a potent family inhibitor with s of 8EGFR IC50pM 49 52 52 nM for EGFR ErbB2 ErbB3 and ErbB4respectively

Bioactivity PD168393 is an potent cell-permeable irreversible EGFRinhibitor with IC50 of 070 nM irreversibly alkylate Cys-773inactive against insulin PDGFR FGFR and PKC target EGFR IC50 07 nM [1] (1) PD 168393 inhibite EGFr autophosphorylationin A431 human epidermoid carcinoma cells with gt9-foldhellip

Bioactivity Pelitinib (EKB-569WAY-EKB 569) is an irreversible inhibitorof with an of 385 nM also slightly inhibits SrcEGFR IC50MEKERK and ErbB2 with s of 282 800 and 1255 nMIC50respectively

NRC-2694 Cat No HY-19909

Olmutinib (HM61713 BI 1482694) Cat No HY-19730

Osimertinib (AZD-9291 Mereletinib) Cat No HY-15772

Osimertinib dimesylate (AZD-9291 (dimesylate) Mereletinib (dimesylate)) Cat No HY-79077

Osimertinib mesylate (AZD-9291 mesylate Mereletinib mesylate) Cat No HY-15772A

PD153035 (SU-5271 AG1517 NSC 669364) Cat No HY-14346

PD153035 Hydrochloride (ZM 252868 AG 1517 SU 5271) Cat No HY-12013

PD158780 Cat No HY-18609

PD168393 Cat No HY-13896

Pelitinib (EKB-569 WAY-EKB 569) Cat No HY-32718

Purity 9916Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9999Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9745Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9830Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9898Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9860Clinical Data No Development ReportedSize 10mM x 1mL in Water

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9884Clinical Data Phase 3Size 1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9992Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9872Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity PF-06459988 is an irreversible inhibitor of T790M-ContainingEGFR Mutants

Bioactivity Poziotinib(NOV120101 HM781-36B) is an irreversible Pan-HERinhibitor with IC50s of 3523 nM for HER1HER2HER4respectively IC50 value 3523 nM(HER1HER2HER4) [1]Target pan-HER inhibitor in vitro The IC50 levels ofHM781-36B for N87 and SNU216 were 0001 and 0004 μmolLhellip

Bioactivity Pyrotinib (SHR-1258) is a potent and selective dualEGFRHER2inhibitor with s of 13 and 38 nM respectivelyIC50

Bioactivity Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent andselective dual inhibitor with s of 13 and 38EGFRHER2 IC50nM respectively

Bioactivity RG13022 is a inhibitor inhibits thetyrosine kinaseautophosphorylation reaction of the EGF receptor with an IC50of 4 μM

Bioactivity RG14620 is an inhibitor with an of 3 μMEGFR IC50

Bioactivity Rociletinib (CO-1686) is an orally delivered kinase inhibitorthat specifically targets the mutant forms of includingEGFRT790M and the values for EGFRL858RT790M and EGFRWT areKi215 nM and 3033 nM respectively

Bioactivity Rociletinib hydrobromide (CO-1686 hydrobromide) is an orallydelivered kinase inhibitor that specifically targets themutant forms of including T790M and the values forEGFR KiEGFRL858RT790M and EGFRWT are 215 nM and 3033 nMrespectively

Bioactivity Sapitinib (AZD-8931) is a reversible ATP competitive EGFRinhibitor of with s of 4 3 and 4 nM for EGFR ErbB2 andIC50ErbB3 in cells respectively

Bioactivity TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor withIC50 of 17 nM and 23 nM gt10-fold selectivity for HER12than HER4 less potent to MEK15 c-Met Aurora B Lck CSKetc

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PF-06459988 Cat No HY-19985

Poziotinib (HM781-36B NOV120101) Cat No HY-15730

Pyrotinib (SHR-1258) Cat No HY-104065

Pyrotinib dimaleate (SHR-1258 dimaleate) Cat No HY-104065B

RG13022 (Tyrphostin RG13022 ) Cat No HY-101429

RG14620 (Tyrphostin RG14620) Cat No HY-101426

Rociletinib (CO-1686 AVL-301 CNX-419) Cat No HY-15729

Rociletinib hydrobromide (CO-1686 (hydrobromide) AVL-301

hydrobromide CNX-419 hydrobromide) Cat No HY-15729A

Sapitinib (AZD-8931) Cat No HY-13050

TAK-285 Cat No HY-15196

wwwMedChemExpresscom 13

Purity 9814Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9887Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9910Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9853Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9930Clinical Data LaunchedSize 1 mg 5 mg 25 mg

Purity 9921Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9955Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9897Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity Tarloxotinib bromide is an irreversible inhibitorEGFRHER2 Bioactivity TAS6417 is an inhibitor and an efficacious drugEGFRcandidate for patients with NSCLC with values rangingIC50from 11-80 nM

Bioactivity Tesevatinib (XL-647) is an orally available multi-targettyrosine kinase inhibitor inhibits EGFR ErbB2 KDR Flt4and kinase with s of 03 16 15 87 and 14 nMEphB4 IC50

Bioactivity Trastuzumab is a humanized monoclonal antibody for patientswith invasive breast cancers that overexpress HER2Trastuzumab has been clinically used to treat HER2 PositiveMetastatic Breast Cancer and HER2 Positive Gastric Cancer

Bioactivity Tucatinib (Irbinitinib ARRY-380 ONT-380) is a potent andselective inhibitor with an of 8 nMHER2 IC50

Bioactivity Tyrphostin 23 (Tyrphostin A23) is an inhibitor with anEGFR and of 35 and 11 μM respectivelyIC50 Ki

Bioactivity Tyrphostin AG 528 is an inhibitor of and withEGFR ErbB2s of 49 and 21 μM respectivelyIC50

Bioactivity TyrphostinAG879 is a tyrosine kinase inhibitor that inhibitsTrKA phosphorylation but not TrKB and TrKC[1] also a ErbB2kinase inhibitor has at least 500-fold higher selectivity toErbB2 (IC50 = 1 μmolL) than EGFR (IC50 gt500 μmolL)target TrKA [1] ErbB2 [2] IC 50 ErbB2 1 μmolL [2] Inhellip

Bioactivity Varlitinib (ARRY-334543 ASLAN001) is a potent reversiblesmall molecule pan- inhibitor with s of 7 2 4 nMEGFR IC50for HER1 HER2 and HER4 respectively

Bioactivity WHI-P154 is a potent inhibitor and also modestly blocksEGFR with s of 4 nM and 18 μM respectivelyJAK3 IC50

tarloxotinib bromide (TH-4000 PR-610) Cat No HY-17632

TAS6417 Cat No HY-112299

Tesevatinib (XL-647 EXEL-7647 KD-019) Cat No HY-13314

Trastuzumab (Anti-Human HER2 Humanized Antibody) Cat No HY-P9907

Tucatinib (Irbinitinib ARRY-380 ONT-380) Cat No HY-16069

Tyrphostin 23 (Tyrphostin A23 RG-50810 AG 18) Cat No HY-15644

Tyrphostin AG 528 (Tyrphostin B66 AG 528) Cat No HY-100499

Tyrphostin AG 879 (AG 879) Cat No HY-20878

Varlitinib (ARRY-334543 ASLAN001) Cat No HY-10530

WHI-P154 Cat No HY-13895

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9867Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9907Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Bioactivity WHI-P180 (Janex 3) is a multi-kinase inhibitor inhibits RET and with s of 5 nM 66 nM and 4 μMKDR EGFR IC50

respectively

Bioactivity WHI-P180 (Janex 3) is a multi-kinase inhibitor inhibits RET and with s of 5 nM 66 nM and 4 μMKDR EGFR IC50

respectively

Bioactivity WZ3146 is a mutant selective inhibitor with s of 2EGFR IC50

2 5 14 and 66 nM for EGFR EGFR EGFRL858R L858RT790M

EGFR and EGFR respectivelyE746_A750 E746_A750T790M

Bioactivity WZ4002 is a mutant selective inhibitor with s of 2EGFR IC50

8 3 and 2 nM for EGFR EGFR EGFRL858R L858RT790M

and EGFR respectivelyE746_A750 E746_A750T790M

Bioactivity WZ8040 is a novel mutant-selective irreversible EGFRT790Minhibitor does not inhibit ERBB2 phosphorylation (T798I)

Bioactivity ZD-4190 is a potent orally available inhibitor of thevascular endothelial cell growth factor receptor 2 ( )VEGFR2and of epidermal growth factor receptor ( ) signallingEGFRused for the treatment of cancer

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WHI-P180 (Janex 3) Cat No HY-15769

WHI-P180 hydrochloride (Janex 3 hydrochloride ) Cat No HY-15769A

WZ-3146 Cat No HY-12001

WZ4002 Cat No HY-12026

WZ8040 Cat No HY-12029

ZD-4190 Cat No HY-U00002

wwwMedChemExpresscom 15

JAKJanus kinase

Janus kinase (JAK) is a family of intracellular nonreceptor tyrosinekinases that transduce cytokine-mediated signals via the JAK-STATpathway Since members of the type I and type II cytokine receptorfamilies possess no catalytic kinase activity they rely on the JAKfamily of tyrosine kinases to phosphorylate and activate downstreamproteins involved in their signal transduction pathways The receptorsexist as paired polypeptides thus exhibiting two intracellularsignal-transducing domains JAKs associate with a proline-rich regionin each intracellular domain which is adjacent to the cell membraneand called a box1box2 region After the receptor associates with itsrespective cytokineligand it goes through a conformational change

bringing the two JAKs close enough to phosphorylate each other The JAK autophosphorylation induces aconformational change within itself enabling it to transduce the intracellular signal by further phosphorylating andactivating transcription factors called STATs The activated STATs dissociate from the receptor and form dimers beforetranslocating to the cell nucleus where they regulate transcription of selected genes

Purity 9970Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9937Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 2 mg 5 mg 10 mg 50 mg

Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9913Clinical Data Phase 2Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg

JAK Inhibitors amp Modulators

Bioactivity (3R4S)-Tofacitinib is an enantiomer of TofacitinibTofacitinib inhibits with of 1 nMJAK3 IC50

Bioactivity (3S4R)-Tofacitinib is an enantiomer of TofacitinibTofacitinib inhibits with of 1 nMJAK3 IC50

Bioactivity (3S4S)-Tofacitinib is the S-enantiomer of TofacitinibTofacitinib inhibits with of 1 nMJAK3 IC50

Bioactivity ASN-002 is a potent dual inhibitor of spleen tyrosine kinase () and janus kinase ( ) with values of 5-46 nMSYK JAK IC50

Bioactivity AT9283 is a multitargeted kinase inhibitor which potentlyinhibits ( =12 nM 11 nM)aurora kinase AB JAK23 IC50

Bioactivity Atractylenolide I is a sesquiterpene derived from the rhizomeof Atractylodes macrocephala possesses diverse bioactivitiessuch as neuroprotective anti-allergic anti-inflammatory andanticancer properties Atractylenolide I reduces proteinlevels of phosphorylated and in A375 cells andhellipJAK2 STAT3

Bioactivity AZ960 is a potent and specific inhibitor of the kinaseJAK2with a of 045 nMKi

Bioactivity AZD-1480 is an ATP-competitive inhibitor of and JAK1 JAK2with s of 13 and lt04nM respectivelyIC50

Bioactivity AZD-4205 is a selective inhibitor with an of 73JAK1 IC50nM weakly inhibits JAK2 and shows little inhibition on JAK3( gt147 gt30 μM respectively)IC50

Bioactivity Baricitinib is a selective and orally bioavailable andJAK1 inhibitor with s of 59 nM and 57 nM respectivelyJAK2 IC50

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(3R4S)-Tofacitinib Cat No HY-40354D

(3S4R)-Tofacitinib Cat No HY-40354B

(3S4S)-Tofacitinib Cat No HY-40354C

ASN-002 Cat No HY-103018

AT9283 Cat No HY-50514

Atractylenolide I Cat No HY-N0201

AZ960 Cat No HY-10411

AZD-1480 (AZD1480 AZD 1480) Cat No HY-10193

AZD-4205 Cat No HY-107361

Baricitinib (INCB028050 LY3009104) Cat No HY-15315

wwwMedChemExpresscom 17

Purity 9862Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9914Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9891Clinical Data Phase 3Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9833Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9900Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9803Clinical Data Phase 2Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9949Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Baricitinib phosphate is a selective orally bioavailable inhibitor with of 59 nM and 57 nMJAK1 JAK2 IC50

respectively

Bioactivity BMS-066 is an pseudokinase inhibitor with of 9IKKβTyk2 IC s50nM and 72 nM respectively

Bioactivity BMS-911543 is a selective inhibitor with s of 11JAK2 IC50nM less selective at JAK1 JAK3 and TYK2 ( 75 360 66IC50nM respectively)

Bioactivity CEP-33779 is a novel selective and orally bioavailableinhibitor of with an of 18plusmn06 nMJAK2 IC50

Bioactivity Cerdulatinib (PRT062070) is a dual and inhibitorJAK SYKwith s of 12 6 8 and 32 for JAK1 2 3 and SYKIC50respectively

Bioactivity CHZ868 is a type II inhibitor with an of 017 μM inJAK2 IC50EPOR JAK2 WT BaF3 cell

Bioactivity Cucurbitacin I is a natural selective inhibitor of with potent anti-cancer activityJAK2STAT3

Bioactivity Decernotinib is a potent orally active inhibitor withJAK3s of 25 11 13 and 11 nM for JAK1 JAK2 and TYK2Ki JAK3

respectively

Bioactivity Delgocitinib is a novel and specific inhibitor with sJAK IC50of 28 26 13 and 58 nM for JAK1 JAK2 JAK3 and Tyk2respectively

Bioactivity Fedratinib (TG-101348) is a selective inhibitor of withJAK2an of 3 nM showing 35- and 334-fold selectivity overIC50JAK1 and JAK3 respectively

Baricitinib phosphate (INCB028050 LY3009104) Cat No HY-15315A

BMS-066 Cat No HY-18710

BMS-911543 Cat No HY-15270

CEP-33779 Cat No HY-15343

Cerdulatinib (PRT062070 PRT2070) Cat No HY-15999

CHZ868 Cat No HY-18960

Cucurbitacin I (Elatericin B JSI-124 NSC-521777) Cat No HY-N1405

Decernotinib (VX-509 VRT-831509) Cat No HY-12469

Delgocitinib (JTE-052) Cat No HY-109053

Fedratinib (TG-101348 SAR 302503) Cat No HY-10409

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9878Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9987Clinical Data Phase 3Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9827Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9800Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9996Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9841Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9964Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity Filgotinib (GLPG0634) is a selective inhibitor with JAK1 IC50of 10 nM 28 nM 810 nM and 116 nM for JAK1 JAK2 JAK3 andTYK2 respectively

Bioactivity FM381 is a potent covalent reversible inhibitor of JAK3targeting the unique Cys909 at the gatekeeper position +7 inJAK3 FM-381 has an of 127 pM for JAK3 with 410 2700IC50and 3600-fold selectivity over JAK1 JAK2 and TYK2respectively

Bioactivity Gandotinib (LY2784544) is a potent inhibitor with JAK2 IC50of 3 nM Gandotinib (LY2784544) also inhibits FLT3 FLT4FGFR2 TYK2 and TRKB with IC of 4 25 32 44 and 95 nM50

Bioactivity GLPG0634 (analog) (compound176)is a pan JAK inhibitor withIC50s of 50-200 nM for JAK1JAK2JAK3 more information can befound in the reference patents

Bioactivity NS-018 is a highly active and orally bioavailable JAK2inhibitor with an of 072 nM 46- 54- and 31-foldIC50selectivity for JAK2 over JAK1 ( 33 nM) JAK3 ( 39IC50 IC50nM) and Tyk2 ( 22 nM)IC50

Bioactivity NS-018 hydrochloride is a highly active and orallybioavailable inhibitor with an of 072 nM 46-JAK2 IC5054- and 31-fold selectivity for JAK2 over JAK1 ( 33IC50nM) JAK3 ( 39 nM) and Tyk2 ( 22 nM)IC50 IC50

Bioactivity Itacitinib is a potent and selective inhibitor of withJAK1gt20-fold selectivity for JAK1 over JAK2 and gt100-foldover JAK3 and TYK2 Itacitinib is used in the research ofmyelofibrosis

Bioactivity Itacitinib adipate is a selective inhibitor which hasJAK1been tested for efficacy and safety in a phase II trial inmyelofibrosis

Bioactivity JAK inhibitor 1 is an inhibitor of extracted from patentJAKUS20170121327A1 compound example 283

Bioactivity JAK-IN-1 is a inhibitor with s of 026 08 andJAK123 IC5032 nM respectively JAK-IN-1 shows improved selectivity forJAK3 over JAK1

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Filgotinib (GLPG0634) Cat No HY-18300

FM381 Cat No HY-102046

Gandotinib (LY2784544) Cat No HY-13034

GLPG0634 analog Cat No HY-13961

Ilginatinib (NS-018) Cat No HY-19631A

Ilginatinib hydrochloride (NS-018 hydrochloride) Cat No HY-19631B

Itacitinib (INCB039110) Cat No HY-16997

Itacitinib adipate Cat No HY-16997A

JAK inhibitor 1 Cat No HY-111471

JAK-IN-1 Cat No HY-13827

wwwMedChemExpresscom 19

Purity 955Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity 9833Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 960Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity 9811Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9984Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9916Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity JAK3-IN-1 is a potent JAK3 inhibitor with IC50 of 48 nM alsoinhibits JAK1 (IC50 = 896 nM) and JAK2 (IC50 = 1050 nM) IC50value 48 nM [1] Target JAK3 in vitro JAK3-IN-1 provides aset of useful tools to pharmacologically interrogateJAK3-dependent biology JAK3-IN-1 completely inhibits IL-4hellip

Bioactivity JAK3-IN-6 is a potent selective irreversible Janus AssociatedKinase 3 (JAK3) inhibitor with an of 015 nMIC50

Bioactivity JAK3-IN-7 is a potent and selective inhibitor extractedJAK3from patent WO2011013785A1 has an of lt001 μMIC50

Bioactivity JANEX-1 is a potent and specific inhibitor (estimatedJAK3=23 μM) JANEX-1 (WHI-P131) shows potent JAK3-inhibitoryKi

activity ( of 78 μM) does not inhibit JAK1 and JAK2IC50

Bioactivity LFM-A13 is a potent inhibitor inhibitsBTK JAK2 PLKrecombinant BTK Plx1 and PLK3 with s of 25 μM 10 μM andIC5061 μM LFM-A13 shows no effects on JAK1 and JAK3 Src familykinase HCK EGFR and IRK

Bioactivity Momelotinib (CYT387) is an ATP-competitive inhibitor of with a of 11 nM and 18 nMrespectively CYT387JAK1JAK2 IC50

shows much less activity against JAK3

Bioactivity Momelotinib Mesylate (CYT387 Mesylate) is an ATP-competitiveinhibitor of with of 11 nM18 nM appr 10-foldJAK1JAK2 IC50selectivity versus JAK3

Bioactivity Momelotinib sulfate (CYT387 sulfate) is an ATP-competitiveinhibitor of with of 11 nM18 nM 10-foldJAK1JAK2 IC50selectivity versus JAK3 (IC =155 nM)50

Bioactivity NS-018 maleate is a highly active and orally bioavailable inhibitor with an of 072 nM 46- 54- andJAK2 IC50

31-fold selectivity for JAK2 over JAK1 ( 33 nM) JAK3 (IC50 39 nM) and Tyk2 ( 22 nM)IC50 IC50

Bioactivity NSC 42834 a novel specific inhibitor of Jak2 inhibitsJak2-V617F and Jak2-WT autophosphorylation in a dose-dependentmanner but was not cytotoxic to cells at concentrations thatinhibited kinase activity

JAK3-IN-1 Cat No HY-19544

JAK3-IN-6 Cat No HY-101976

JAK3-IN-7 Cat No HY-U00390

JANEX-1 (WHI-P131 Jak3 inhibitor I) Cat No HY-15508

LFM-A13 Cat No HY-18009

Momelotinib (CYT387) Cat No HY-10961

Momelotinib Mesylate (CYT387 (Mesylate)) Cat No HY-10963

Momelotinib sulfate (CYT387 (sulfate salt)) Cat No HY-10962

NS-018 maleate Cat No HY-19631

NSC 42834 (JAK2 Inhibitor V Z3) Cat No HY-15480

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg 1 g

Purity 9955Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 1Size 5 mg 10 mg 50 mg 100 mg

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9943Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9966Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9953Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9800Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Bioactivity NVP-BSK805 is an ATP-competitive inhibitor with sJAK2 IC50of 048 nM 3163 nM 1868 nM and 1076 nM for JAK2 JH1 (JAKhomology 1) JAK1 JH1 JAK3 JH1 and TYK2 JH1 respectively

Bioactivity NVP-BSK805 dihydrochloride is an ATP-competitive JAK2inhibitor with s of 048 nM 3163 nM 1868 nM andIC501076 nM for JAK2 JH1 (JAK homology 1) JAK1 JH1 JAK3 JH1and TYK2 JH1 respectively

Bioactivity Oclacitinib maleate is a novel inhibitor Oclacitinib isJAKmost potent at inhibiting ( =10 nM)JAK1 IC50

Bioactivity Pacritinib is a potent inhibitor of both wild-type (ICJAK2=23 nM) and mutant (IC =19 nM) Pacritinib50 JAK2V617F

50

also inhibits (IC =22 nM) and its mutant FLT3 50 FLT3D835Y

(IC =6 nM)50

Bioactivity Peficitinib is an oral inhibitor with s of 39 50JAK IC5007 and 48 nM for JAK1 JAK2 JAK3 and Tyk2 respectively

Bioactivity PF-06651600 is a potent -selective inhibitor with an JAK3 IC50of 331 nM

Bioactivity Pyridone 6 is a inhibitor which potently inhibitspan-JAKthe JAK kinase family with s of 1 nM for and IC50 JAK2 TYK2

5 nM for and 15 nM for while displayingJAK3 JAK1significantly weaker affinities (130 nM to gt10 mM) forother protein tyrosine kinases

Bioactivity RGB-286638 is a inhibitor that inhibits the kinaseCDKactivity of cyclin T1-CDK9 cyclin B1-CDK1 cyclin E-CDK2

and with s of 1cyclin D1-CDK4 cyclin E-CDK3 p35-CDK5 IC502 3 4 5 and 5 nM respectively also inhibits GSK-3β TAhellip

Bioactivity RGB-286638 is a inhibitor that inhibits the kinaseCDKactivity of cyclin T1-CDK9 cyclin B1-CDK1 cyclin E-CDK2

and with s of 1cyclin D1-CDK4 cyclin E-CDK3 p35-CDK5 IC502 3 4 5 and 5 nM respectively also inhibits GSK-3β TAhellip

Bioactivity Ruxolitinib is a potent and selective inhibitor withJAK12s of 33 nM and 28 nM in cell-free assays and hasIC50

130-fold selectivity for JAK12 over JAK3

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NVP-BSK805 (BSK 805) Cat No HY-14722

NVP-BSK805 dihydrochloride (BSK805 dihydrochloride) Cat No HY-14722A

Oclacitinib maleate (PF-03394197 maleate) Cat No HY-13577A

Pacritinib (SB1518) Cat No HY-16379

Peficitinib (ASP015K JNJ-54781532) Cat No HY-19568

PF-06651600 Cat No HY-100754

Pyridone 6 (CMP 6 JAK Inhibitor) Cat No HY-14435

RGB-286638 Cat No HY-15504

RGB-286638 free base Cat No HY-15504A

Ruxolitinib (INCB018424) Cat No HY-50856

wwwMedChemExpresscom 21

Purity 9941Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9992Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9996Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9894Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9985Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9700Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 9988Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg

Purity 9989Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg 1 g

Bioactivity Ruxolitinib phosphate is a potent inhibitor with sJAK12 IC50of 33 nM28 nM respectively showing more than 130-foldselectivity over JAK3

Bioactivity Ruxolitinib S enantiomer is the S-enantiomer of RuxolitinibRuxolitinib is the first potent selective inhibitorJAK12to enter the clinic with of 33 nM28 nM in cell-freeIC50assays

Bioactivity Ruxolitinib sulfate is the first potent selective JAK12inhibitor to enter the clinic with s of 33 nM28 nM andIC50has gt 130-fold selectivity for JAK12 versus JAK3

Bioactivity SAR-20347 is an inhibitor of and TYK2 JAK1 JAK2 JAK3with s of 06 23 26 and 41 nM respectivelyIC50

Bioactivity SB1317 is a potent inhibitor of and forCDK2 JAK2 FLT3the treatment of cancer with of 13 73 and 56 nM forIC50CDK2 JAK2 and FLT3 respectively

Bioactivity Solcitinib is an orally active competitive potent selective inhibitor with an of 98 nM and 11- 55- andJAK1 IC50

23-fold selectivity over JAK2 JAK3 and TYK2 respectivelySolcitinib is used in the research of moderate-to-severeplaque-type psoriasis

Bioactivity TG101209 is a selective inhibitor with of 6 nMJAK2 IC50less potent to and with of 25 nM and 17 nM apprFlt3 RET IC5030-fold selective for JAK2 than JAK3 and sensitive toJAK2V617F and MPLW515LK mutations

Bioactivity Tofacitinib is a inhibitor with s of 1 20 andJAK123 IC50112 nM respectively

Bioactivity Tofacitinib citrate is a inhibitor with s of 1JAK123 IC5020 and 112 nM respectively

Bioactivity TYK2-IN-2 is an inhibitor of used for treatment ofTYK2inflammatory and autoimmune diseases

Ruxolitinib phosphate (INCB018424 phosphate) Cat No HY-50858

Ruxolitinib S enantiomer (S-Ruxolitinib INCB18424) Cat No HY-50856A

Ruxolitinib sulfate (INCB018424 sulfate) Cat No HY-50859

SAR-20347 Cat No HY-100895

SB1317 (TG02) Cat No HY-15166

Solcitinib (GSK-2586184 GLPG-0778) Cat No HY-16755

TG101209 Cat No HY-10410

Tofacitinib (Tasocitinib CP-690550) Cat No HY-40354

Tofacitinib citrate (Tasocitinib citrate CP-690550 citrate) Cat No HY-40354A

TYK2-IN-2 Cat No HY-101762

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

Purity 980Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9967Clinical Data Phase 1Size 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9948Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9814Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9996Clinical Data Phase 3Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg 200 mg500 mg 1 g 5 g 10 g

Purity 9976Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity Tyk2-IN-3 is a inhibitor with an ofTyk2 pseudokinase IC50485 nM

Bioactivity Tyk2-IN-4 is a selective potent allosteric inhibitor oftyrosine kinase 2 ( )Tyk2

Bioactivity Upadacitinib (ABT-494) is a potent and selective Janus kinase( ) 1 inhibitor with an of 43 nM being developed forJAK IC50the treatment of several autoimmune disorders

Bioactivity WHI-P154 is a potent inhibitor and also modestly blocksEGFR with s of 4 nM and 18 μM respectivelyJAK3 IC50

Bioactivity WHI-P97 is a rationally designed potent inhibitor of JAK-3IC50 value Target JAK3 Treatment of mast cells with WHI-P97inhibited the translocation of 5-lipoxygenase (5-LO) from thenucleoplasm to the nuclear membrane and consequently5-LO-dependent leukotriene (LT) synthesis after IgEhellip

Bioactivity WP1066 is an inhibitor of and and also showsJAK2 STAT3effect on STAT5 and ERK12 without affecting JAK1 and JAK3

Bioactivity XL019 is a potent and selective JAK2 inhibitor with IC50 of22 nM 100 fold selectivity over JAK1 shows good biochemicaland cellular potency against JAK2 with good selectivityagainst the Janus Kinase family as well as a broad kinasepanel IC50 Value 22 nM (JAK2) 2142 nM (JAK3) [1] XL019hellip

Bioactivity ZM39923 is a inhibitor with a of 71 ZM39923JAK3 pIC50also potently inhibits tissue transglutaminase ( ) withTGM2an of 10 nMIC50

Bioactivity ZM39923 hydrochloride is a inhibitor with a ofJAK3 pIC5071 ZM39923 hydrochloride also potently inhibits tissuetransglutaminase ( ) with an of 10 nMTGM2 IC50

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Tyk2-IN-3 Cat No HY-18709

Tyk2-IN-4 Cat No HY-117287

Upadacitinib (ABT-494) Cat No HY-19569

WHI-P154 Cat No HY-13895

WHI-P97 Cat No HY-11067

WP1066 Cat No HY-15312

XL019 Cat No HY-13775

ZM39923 Cat No HY-12589A

ZM39923 hydrochloride Cat No HY-12589

wwwMedChemExpresscom 23

PimPim kinases

Pim kinases are a small family of serinethreonine kinases regulatingseveral signaling pathways that are fundamental to cancerdevelopment and progression They were first recognized as pro-viralintegration sites for the Moloney Murine Leukemia virus Pim kinasespossess a hinge region which creates a unique binding pocket forATP Absence of a regulatory domain means that these proteins areconstitutively active once transcribed Pim kinases are criticaldownstream effectors of the ABL (ableson) JAK2 (janus kinase 2) andFlt-3 (FMS related tyrosine kinase 1) oncogenes and are required bythem to drive tumorigenesis Recent investigations have establishedthat the Pim kinases function as effective inhibitors of apoptosis and

when overexpressed produce resistance to the mTOR (mammalian target of rapamycin) inhibitor rapamycin Overexpression of the PIM kinases has been reported in several hematological and solid tumors (PIM 1) myelomalymphoma leukemia (PIM 2) and adenocarcinomas (PIM 3) As such the Pim kinases are a very attractive target forpharmacological inhibition in cancer therapy Novel small molecule inhibitors of the human Pim kinases have beendesigned and are currently undergoing preclinical evaluation

Purity 9991Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9933Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9849Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9955Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9913Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9967Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity 9621Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg

Pim Inhibitors amp Modulators

Bioactivity (1S3R5R)-PIM447 (dihydrochloride) an inhibitorPIMextracted from patent US 20100056576 A1 compound example 72has values of 0095 μM for Pim1 0522 μM for Pim2 andIC500369 μM for Pim3

Bioactivity (Z)-SMI-4a is a selective ATP-competitive Pim-1 kinaseinhibitor with an IC50 of 21 nM for Pim-1 compared to an IC50of 100 nM for Pim-2 and with little or no activity against apanel of 50 other kinases tested IC50 value 21 nM (Pim1)100 nM (Pim2) [1] Target Pim-1 in vitro Incubation ofhellip

Bioactivity AZD1208 is a novel orally bioavailable highly selective kinases inhibitorPIM

Bioactivity AZD1208 hydrochloride is a novel orally bioavailable highlyselective kinases inhibitorPIM

Bioactivity CX-6258 is a potent orally efficacious Pim 123kinase(IC50=5 nM25 nM16 nM) inhibitor with excellentbiochemical potency and kinase selectivity

Bioactivity CX-6258 hydrochloride hydrate is a potent orally efficaciousPim 123 kinase(IC50=5 nM25 nM16 nM) inhibitor withexcellent biochemical potency and kinase selectivity

Bioactivity GDC-0339 is a Pim kinase inhibitor with IC50 of 436 nM forBaF3 PIM1 IC50 value 436 nM (for BaF3 PIM1) 004 nM (Kifor PIM1 LC-3K) Target Pim

Bioactivity GNE-955 is a potent pan inhibitor with s of 18Pim kinase Ki110 8 nM for Pim1 Pim2 Pim3 respectively

Bioactivity Hispidulin is a natural flavone with a broad spectrum ofbiological activities Hispidulin is a Pim-1 inhibitor with an

of 271 μMIC50

Bioactivity INCB053914 phosphate is an inhibitor of extracted fromPimpatent WO 2017044730 A1 compound 1 has an of less thanIC5035 nM

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(1S3R5R)-PIM447 dihydrochloride ((1S3R5R)-LGH447 dihydrochloride) Cat No HY-19322C

(Z)-SMI-4a Cat No HY-16576A

AZD1208 Cat No HY-15604

AZD1208 hydrochloride Cat No HY-15604A

CX-6258 Cat No HY-18095

CX-6258 hydrochloride hydrate Cat No HY-18095A

GDC-0339 Cat No HY-16976

GNE-955 Cat No HY-101783

Hispidulin (Dinatin) Cat No HY-N1950

INCB053914 phosphate Cat No HY-101870B

wwwMedChemExpresscom 25

Purity 9971Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9741Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9994Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize

Purity gt98Clinical Data Phase 2Size 1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9810Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9967Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Bioactivity M-110 is a novel and highly selective inhibitor of PIMkinases inhibits the proliferation of prostate cancer celllines with IC50s of 06 to 09 uM with no activity on normalhuman peripheral blood mononuclear cells up to 40 uM

Bioactivity PIM447 is a ihibitor with s of 6 18 9 nMpan-PIM kinase Kifor PIM1 PIM2 and PIM3 respectively

Bioactivity Pim1AKK1-IN-1 is a potent multi-kinase inhibitor with Kdvalues of 35 nM53 nM75 nM380 nM for Pim1AKK1MST2LKB1respectively and also inhibits MPSK1 and TNIK

Bioactivity PIM447 is novel pan-PIM kinase inhibitor including MoloneyMurine Leukemia (PIM) 1 2 and 3 Kinase

Bioactivity Quercetagetin (6-Hydroxyquercetin) is the major flavonoidisolated from ( ) peel QuercetagetinCitrus unshiu C unshiu [3]

is a moderately potent and selective cell-permeable pim-1kinase inhibitor ( 034 μM) Anti-inflammatory hellipIC50

[1]

Bioactivity SGI-1776 is an inhibitor of kinases with s of 7Pim IC50nM 363 nM and 69 nM for Pim-1 -2 and -3 respectively

Bioactivity SMI-16a is a selective kinase inhibitor with Pim IC50values of 015 002 and 48 μM for Pim1 Pim2 and PC3 cellsrespectively

Bioactivity TCS PIM-1 1(sc-204330) is a potent and selectiveATP-competitive Pim-1 kianse inhibitor with IC50 of 50 nMdisplays good selectivity over Pim-2 and MEK1MEK2(IC50sgt20000 nM) IC50 value 50 nM [1] Target Pim-1 TCS PIM-11 bound convincingly within the ATP-binding site of Pim-1hellip

Bioactivity TCS-PIM-1-4a is a Pim inhibitor that blocks mTORC1 activityvia activation of AMPK kills a wide range of both myeloid andlymphoid cell lines (with IC50 values ranging from 08 to 40μM) IC50 value Target Pim SMI-4a a novelbenzylidene-thiazolidine-2 4-dione small molecule inhibitorhellip

Bioactivity TP-3654 is a second-generation kinase inhibitor with Pim Kivalues of 5 and 42 nM for Pim-1 and Pim-3 respectively

M-110 Cat No HY-12830

PIM-447 dihydrochloride (LGH447 dihydrochloride) Cat No HY-19322B

Pim1AKK1-IN-1 (LKB1AAK1 dual inhibitor) Cat No HY-10371

PIM447 (LGH447) Cat No HY-19322

Quercetagetin (6-Hydroxyquercetin) Cat No HY-N4149

SGI-1776 Cat No HY-13287

SMI-16a (PIM12 Kinase Inhibitor VI) Cat No HY-101947

TCS PIM-1 1 (SC 204330) Cat No HY-18086

TCS-PIM-1-4a (SMI-4a) Cat No HY-16576

TP-3654 Cat No HY-101126

STAT

STAT is a family of cytoplasmic protein that regulates many aspects ofgrowth survival and differentiation in cells The transcription factorsof this family are activated by Janus kinase and dysregulation of thispathway is frequently observed in primary tumours and leads toincreased angiogenesis enhanced survival of tumours andimmunosuppression Gene knockout studies have provided evidencethat STAT proteins are involved in the development and function ofthe immune system and play a role in maintaining immune toleranceand tumour surveillance STAT proteins were originally described aslatent cytoplasmic transcription factors that require phosphorylationfor nuclear retention The unphosphorylated STAT proteins shuttle

between cytosol and the nucleus waiting for its activation signal Once the activated transcription factor reaches thenucleus it binds to consensus DNA-recognition motif called gamma-activated sites (GAS) in the promoter region ofcytokine-inducible genes and activates transcription of these genes

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wwwMedChemExpresscom 27

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg

Purity 9811Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9923Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 250 mg 500 mg

Purity 9920Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9917Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9984Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

STAT Inhibitors amp Modulators

Bioactivity AG-490 is a tyrosine kinase inhibitor that inhibits EGFR and Stat-3 JAK23

Bioactivity Alantolactone is a selective inhibitor with potentSTAT3anticancer activity

Bioactivity Artesunate is an inhibitor of both and STAT-3 exported ( )protein 1 EXP1

Bioactivity AS1517499 is a potent inhibitor with an of 21 nMSTAT6 IC50

Bioactivity Atractylenolide I is a sesquiterpene derived from the rhizomeof Atractylodes macrocephala possesses diverse bioactivitiessuch as neuroprotective anti-allergic anti-inflammatory andanticancer properties Atractylenolide I reduces proteinlevels of phosphorylated and in A375 cells andhellipJAK2 STAT3

Bioactivity Balsalazide could suppress colitis-associated carcinogenesisthrough modulation of pathwayIL-6STAT3

Bioactivity Balsalazide sodium hydrate could suppress colitis-associatedcarcinogenesis through modulation of pathwayIL-6STAT3

Bioactivity BP-1-102 is an orally available small-molecule inhibitor oftranscription factor with an of 68 μMStat3 IC50

Bioactivity C188-9 is a inhibitor with a of 47 nMStat3 Kd Bioactivity Casticin is a methyoxylated flavonol isolated from Viticis with antimitotic and anti-inflammatory effectFructus

Casticin inhibits the activation of STAT3

AG-490 (Tyrphostin AG 490) Cat No HY-12000

Alantolactone ((+)-Alantolactone Alant camphor Inula camphor) Cat No HY-N0038

Artesunate Cat No HY-N0193

AS1517499 Cat No HY-100614

Atractylenolide I Cat No HY-N0201

Balsalazide Cat No HY-B0667

Balsalazide sodium hydrate (Balsalazide disodium dihydrate) Cat No HY-B0667A

BP-1-102 Cat No HY-100493

C188-9 Cat No HY-112288

Casticin (Vitexicarpin) Cat No HY-N0516

Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 980Clinical Data No Development ReportedSize 50 mg

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9851Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9975Clinical Data No Development ReportedSize 5 mg 10 mg

Purity 9529Clinical Data No Development ReportedSize 500u g 1 mg

Purity gt98Clinical Data No Development ReportedSize 500u g 1 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

Bioactivity CMD178 is a lead peptide that consistently reduced theexpression of Foxp3 and STAT5 induced by IL-2s IL-2Rαsignaling CMD178 also is an inhibitor of STAT5 and inhibit T

cell development reg[1]

Bioactivity Colivelin is a neuroprotective peptide and activator ofSTAT3

Bioactivity Colivelin (TFA) is a neuroprotective peptide and activator ofSTAT3

Bioactivity Corylifol A inhibits IL-6-induced activation andSTAT3phosphorylation with an of 081 μMIC50

Bioactivity Cryptotanshinone is a natural compound extracted from the rootof Bunge that shows antitumorSalvia miltiorrhizaactivities Cryptotanshinone inhibits with an ofSTAT3 IC5046 μM

Bioactivity Cucurbitacin I is a natural selective inhibitor of with potent anti-cancer activityJAK2STAT3

Bioactivity Dihydroisotanshinone I is a bioactive compound present in awidely used traditional Chinese medicine named danshen

Bioactivity Diosgenin a steroidal saponin can inhibit signalingSTAT3pathway

Bioactivity ENMD-119 is a 2-methoxyestradiol analogue withantiproliferative and antiangiogenic activity and is suitablefor inhibiting HIF-1α and STAT3 in human HCC cells

Bioactivity HJC0152 hydrochloride is a signal transducers and activators of ( ) inhibitortranscription 3 STAT3

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CMD178 Cat No HY-P1453

Colivelin Cat No HY-P1061

Colivelin TFA Cat No HY-P1061A

Corylifol A (Corylifol-A Corylinin) Cat No HY-N0897

Cryptotanshinone (Cryptotanshinon Tanshinone c) Cat No HY-N0174

Cucurbitacin I (Elatericin B JSI-124 NSC-521777) Cat No HY-N1405

Dihydroisotanshinone I Cat No HY-B1919

Diosgenin Cat No HY-N0177

ENMD-119 (ENMD 1198 IRC 110160) Cat No HY-16196

HJC0152 hydrochloride Cat No HY-100602

wwwMedChemExpresscom 29

Purity 9920Clinical Data LaunchedSize 10mM x 1mL in DMSO

200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 5 g 10 g

Purity 9500Clinical Data LaunchedSize 10mM x 1mL in DMF

5 g 10 g

Purity 980Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg 1 g

Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg

Purity 9806Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9939Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9938Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Bioactivity HO-3867 is a selective and potent inhibitor and showsSTAT3good antitumor activity

Bioactivity Homoharringtonine (Omacetaxine mepesuccinateHHT) is acytotoxic alkaloid with antitumor properties which acts byinhibiting translation elongation

Bioactivity inS3-54A18 is a potent inhibitor with anti-cancerSTAT3properties

Bioactivity Isocryptotanshinone is a potent signal transducer andactivator of transcription 3 ( ) and protein tyrosineSTAT3phosphatase 1B inhibitor with an of 561 μM forPTP1B IC50PTP1B

Bioactivity Mogrol is a biometabolite of mogrosides and acts viainhibition of the and pathways or reducingERK12 STAT3

activation and activating signalingCREB AMPK

Bioactivity Morusin is a prenylated flavonoid isolated from M australiswith various biological activities such as antitumorantioxidant and anti-bacteria property Morusin could inhibit

and activityNF-κB STAT3

Bioactivity Napabucasin is a inhibitor which blocks stem cellSTAT3activity in cancer cells

Bioactivity Niclosamide is an orally bioavailable chlorinatedsalicylanilide with anthelmintic and potential antineoplasticactivity Niclosamide inhibits with of 025 μM inSTAT3 IC50HeLa cells and inhibits DNA replication in a cell-free assay

Bioactivity Niclosamide monohydrate is an inhibitor of with ofSTAT3 IC50025 μM in HeLa cells and inhibits DNA replication in acell-free assay

Bioactivity Nifuroxazide is an effective inhibitor of also exertsSTAT3potent anti-tumor and anti-metastasis activity

HO-3867 Cat No HY-100453

Homoharringtonine (Omacetaxine mepesuccinate HHT) Cat No HY-14944

inS3-54A18 Cat No HY-103128

Isocryptotanshinone Cat No HY-N6651

Mogrol Cat No HY-N2312

Morusin (Mulberrochromene) Cat No HY-N0622

Napabucasin Cat No HY-13919

Niclosamide (BAY2353) Cat No HY-B0497

Niclosamide monohydrate (BAY2353 monohydrate) Cat No HY-B0497B

Nifuroxazide Cat No HY-B1436

Purity 9967Clinical Data Phase 1Size 10mM x 1mL in DMSO

10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 25 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9988Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg

Purity 9890Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity NSC 74859 is a selective inhibitor with an ofStat3 IC5086plusmn33 μM

Bioactivity Pimozide is a antagonist with s ofdopamine receptor Ki14 nM 25 nM and 588 nM for dopamine D2 D3 and D1receptors respectively and also has affinity at

with a of 39 nM Pimozide also inhibhellipα1-adrenoceptor Ki

Bioactivity Saikosaponin D is a triterpene saponin isolated fromBupleurum with anti-inflammatory anti-bacterial anti-tumorand anti-allergic activities Saikosaponin D inhibits selectin

and and activates STAT3 NF-kB estrogen receptor-β

Bioactivity Scutellarin an active flavone isolated from Scutellariabaicalensis can down-regulates the signalingSTAT3GirdinAktin HCC cells and inhibits RANKL-mediated MAPK and NF-κBsignaling pathway in osteoclasts

Bioactivity SH-4-54 is a inhibitor that binds to STAT3 and STAT5STATwith of 300 464 nM respectivelyK sD

Bioactivity SH5-07 is a hydroxamic acid based inhibitor with anStat3 of 39 μM in assayIC50 in vitro

Bioactivity STAT5-IN-1 is a inhibitor with an of 47 μM forSTAT5 IC50STAT5β isoform

Bioactivity Stattic is a potent inhibitor of activation andSTAT3dimerization

Bioactivity WP1066 is an inhibitor of and and also showsJAK2 STAT3effect on STAT5 and ERK12 without affecting JAK1 and JAK3

30 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

NSC 74859 (S3I-201) Cat No HY-15146

Pimozide (R6238) Cat No HY-12987

Saikosaponin D Cat No HY-N0250

Scutellarin Cat No HY-N0751

SH-4-54 Cat No HY-16975

SH5-07 Cat No HY-100494

STAT5-IN-1 Cat No HY-101853

Stattic Cat No HY-13818

WP1066 Cat No HY-15312