Antibody-drug Conjugate/ADC Related...Antibody-drug conjugates. Bioactivity: Auristatin F is a...

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Antibody-drug Conjugate/ADC Related

The antibody-drug conjugate (ADC), a humanized or human monoclonal antibody conjugated with highly cytotoxic smallmolecules (payloads) through chemical linkers, is a novel therapeutic format and has great potential to make a paradigmshift in cancer chemotherapy. The three components of the ADC together give rise to a powerful oncolytic agent capableof delivering normally intolerable cytotoxins directly to cancer cells, which then internalize and release the cell-destroyingdrugs. At present, two ADCs, Adcetris and Kadcyla, have received regulatory approval with >40 others in clinicaldevelopment.ADCs are administered intravenously in order to prevent the mAb from being destroyed by gastric acids and proteolyticenzymes. The mAb component of the ADC enables it to circulate in the bloodstream until it finds and binds totumor-specific cell surface antigens present on target cancer cells. Linker chemistry is an important determinant of thesafety, specificity, potency and activity of ADCs. Linkers are designed to be stable in the blood stream (to conform to theincreased circulation time of mAbs) and labile at the cancer site to allow rapid release of the cytotoxic drug. Firstgeneration ADCs made use of early cytotoxins such as the anthracycline, doxorubicin or the anti-metabolite/antifolateagent, methotrexate. Current cytotoxins have far greater potency and can be divided into three main groups: auristatins,maytansines and calicheamicins.The development of site-specific conjugation methodologies for constructing homogeneous ADCs is an especiallypromising path to improving ADC design, which will open the way for novel cancer therapeutics. References:[1] Tsuchikama K, et al. Protein Cell. 2016 Oct 14. DOI:10.1007/s13238-016-0323-0.

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• ADC Cytotoxin 3

• ADC Linker 8

• Drug-Linker Conjugates for ADC 11

• PROTAC-linker Conjugate for PAC 15

Inhibitors, Agonists, Screening Librarieswww.MedChemExpress.com

Target List in Antibody-drug Conjugate/ADC Related

2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

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ADC Cytotoxin

ADC Cytotoxin are a large collection of toxins for antibody-drugconjugate (ADC) development projects. The toxins that can be usedas payloads should be soluble, amenable to conjugation, and stable.There are myriads of cellular toxins in natural or synthesized, but onlya few have been found adaptable for an ADC concept.The toxins targeting tubulin filaments include Maytansinoids,Auristatins, Taxol derivatives, etc. Amatoxins are a class oftranscription-inhibiting agents. They bind to RNA polymerase II,leading to cell apoptosis. Protein toxins function in the similar MOA(mechanism of action) with cellular toxins, they could inhibit proteinsynthesis and induce cell death. While enzyme-based ADCs alter the

microenvironment of disease tissues to disturb their functions.

https://www.MedChemExpress.com/Targets/ADC Cytotoxin.html

Purity: 98.0%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

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Purity: 98.26%Clinical Data: Phase 4Size: 10mM x 1mL in DMSO,

100 mg, 500 mg


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1 mg, 5 mg, 10 mg


1 mg, 5 mg, 10 mg


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Purity: 99.79%Clinical Data: No Development ReportedSize: 1 mg, 2 mg, 5 mg

Purity: 92.43%Clinical Data: Phase 3Size: 5 mg, 10 mg, 50 mg, 100 mg

Purity: >98%Clinical Data: No Development ReportedSize: 10 mg, 50 mg

ADC Cytotoxin Inhibitors & Modulators

Bioactivity: 10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel derivativewith improved pharmacological features and higher watersolubility. IC50 value: Target: Microtubule inhibitor10-Deacetyl-7-xylosyl paclitaxel induced mitotic cell cyclearrest and apoptosis as measured by flow cytometry, DNA…

Bioactivity: Aldoxorubicin (INNO-206) is an albumin-binding prodrug ofdoxorubicin, which is released from albumin under acidicconditions. Aldoxorubicin (INNO-206) has potent antitumoractivities in various cancer cell lines and in murine tumormodels.

Bioactivity: alpha-Amanitin is the principal toxin of several deadlypoisonous mushrooms, exerting its toxic function by inhibiting

.RNA-polymerase II

Bioactivity: Ansamitocin P 3' exhibits antitumour activity, is an antibodydrug conjugate cytotoxin. The more information please refer toAnsamitocin P-3 (HY-15739).

Bioactivity: Ansamitocin P-3 is a inhibitor. Ansamitocin P-3microtubuleis a macrocyclic antitumor antibiotic.

Bioactivity: Auristatin E is a cytotoxic tubulin modifier with potent andselective antitumor activity; MMAE analog and cytotoxin inAntibody-drug conjugates.

Bioactivity: Auristatin F is a cytotoxic tubulin modifier with potent andselective antitumor activity; MMAF analog and cytotoxin inAntibody-drug conjugates.

Bioactivity: Calicheamicin is a cytotoxic agent that causes double-strandDNA breaks.

Bioactivity: Campathecin is a potent DNA enzyme topoisomerase Iinhibitor, with an of 679 nM.IC50

Bioactivity: D8-MMAD is a deuterated form of MMAD, which is a disrupting agent.microtubule


10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol; 10-Deacetylpaclitaxel 7-Xyloside; …) Cat. No.: HY-20584

Aldoxorubicin (INNO-206; DOXO-EMCH) Cat. No.: HY-16261

alpha-Amanitin (α-Amanitin; α-Amatoxin) Cat. No.: HY-19610

Ansamitocin P 3' (Antibiotic C 15003P3'; Maytansinol butyrate) Cat. No.: HY-19839

Ansamitocin P-3 (Antibiotic C 15003P3; Maytansinol isobutyrate) Cat. No.: HY-15739

Auristatin E Cat. No.: HY-15582

Auristatin F Cat. No.: HY-15583

Calicheamicin (Calicheamicin γ1) Cat. No.: HY-19609

Campathecin (Camptothecin; (S)-(+)-Camptothecin; CPT) Cat. No.: HY-16560

D8-MMAD (Demethyldolastatin 10 D8; Monomethylauristatin D D8; Monomethyl Dolastatin 10 D8) Cat. No.: HY-15581S

https://www.MedChemExpress.com/Targets/ADC Cytotoxin.htmlhttps://www.MedChemExpress.com/10-deacetyl-7-xylosyl-paclitaxel.htmlhttps://www.MedChemExpress.com/INNO-206.htmlhttps://www.MedChemExpress.com/alpha-Amanitin.htmlhttps://www.MedChemExpress.com/Ansamitocin-P-3_acute_.htmlhttps://www.MedChemExpress.com/Ansamitocin-P-3.htmlhttps://www.MedChemExpress.com/Auristatin-E.htmlhttps://www.MedChemExpress.com/Auristatin-F.htmlhttps://www.MedChemExpress.com/Calicheamicin.htmlhttps://www.MedChemExpress.com/Campathecin.htmlhttps://www.MedChemExpress.com/D8-MMAD.html



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Purity: 99.47%Clinical Data: LaunchedSize: 10mM x 1mL in DMSO,

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Purity: >98%Clinical Data: LaunchedSize: 50 mg, 100 mg, 200 mg, 500 mg

Purity: 99.83%Clinical Data: Phase 2Size: 1 mg, 5 mg

Purity: 99.27%Clinical Data: LaunchedSize: 10mM x 1mL in Water,

10 mg, 50 mg, 100 mg, 200 mg, 500 mg

Purity: >98%Clinical Data: LaunchedSize: 10 mg, 50 mg


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1 mg, 5 mg, 10 mg

Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg


Bioactivity: D8-MMAE is a deuterated labeled MMAE, a potent mitoticinhibitor.

Bioactivity: D8-MMAF is a deuterated form of MMAF, which is a disrupting agent.microtubule

Bioactivity: D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride, which is a disrupting agent.microtubule

Bioactivity: Daun02 is a prodrug of the inhibitortopoisomeraseDaunorubicin.

Bioactivity: Daunorubicin (RP 13057, Daunomycin, Rubidomycin) is a inhibitor with potent antineoplastictopoisomerase II

activities. Daunorubicin inhibites inDNA and RNA synthesissensitive and resistant Ehrlich ascites tumor cells.

Bioactivity: Daunorubicin Hydrochloride is a inhibitortopoisomerase IIwith potent antineoplastic activities. DaunorubicinHydrochloride inhibites in sensitive andDNA and RNA synthesisresistant Ehrlich ascites tumor cells.

Bioactivity: Angiotensin II human is a vasoconstrictor that acts on the and the receptor.AT1 AT2

Bioactivity: Doxorubicin is a cytotoxic anthracycline antibiotic for thetreatment of multiple cancers. The possible mechanisms bywhich doxorubicin acts in the cancer cell are intercalationinto DNA and disruption of -mediated DNAtopoisomerase-IIrepair.

Bioactivity: Doxorubicin hydrochloride is a cytotoxic anthracyclineantibiotic for the treatment of multiple cancers. The possiblemechanisms by which doxorubicin acts in the cancer cell areintercalation into DNA and disruption of

-mediated DNA repair.topoisomerase-II

Bioactivity: Duocarmycin TM is an exceptionally potent antitumorantibiotic.

D8-MMAE (D8-Monomethyl auristatin E) Cat. No.: HY-15162A

D8-MMAF (Monomethylauristatin F D8) Cat. No.: HY-15579S

D8-MMAF hydrochloride Cat. No.: HY-15579AS

Daun02 Cat. No.: HY-13061

Daunorubicin (RP 13057; Daunomycin; Rubidomycin) Cat. No.: HY-13062A

Daunorubicin Hydrochloride (RP 13057 (Hydrochloride); Daunomycin (Hydrochloride); Rubidomycin (Hydrochloride)) Cat. No.: HY-13062

Dolastatin 10 (DLS 10; NSC 376128) Cat. No.: HY-15580

Doxorubicin (Hydroxydaunorubicin) Cat. No.: HY-15142A

Doxorubicin hydrochloride (Hydroxydaunorubicin (hydrochloride)) Cat. No.: HY-15142

Duocarmycin TM Cat. No.: HY-107769

https://www.MedChemExpress.com/d8-mmae.htmlhttps://www.MedChemExpress.com/D8-MMAF.htmlhttps://www.MedChemExpress.com/D8-MMAF_hydrochloride.htmlhttps://www.MedChemExpress.com/daun02.htmlhttps://www.MedChemExpress.com/daunorubicin.htmlhttps://www.MedChemExpress.com/Daunorubicin-Hydrochloride.htmlhttps://www.MedChemExpress.com/Dolastatin-10.htmlhttps://www.MedChemExpress.com/Doxorubicin.htmlhttps://www.MedChemExpress.com/Doxorubicin-hydrochloride.htmlhttps://www.MedChemExpress.com/Duocarmycin_TM.html


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Purity: 98.74%Clinical Data: Phase 2Size: 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Purity: >98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg, 100 mg

Purity: >98%Clinical Data: Phase 3Size: 5 mg, 10 mg, 50 mg, 100 mg


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Bioactivity: Dxd is a potent inhibitor, with an ofDNA topoisomerase I IC500.31 μM, used as a conjugated drug of HER2-targeting ADC(DS-8201a).

Bioactivity: Maytansinol inhibits microtubule assembly and inducesmicrotubule disassembly in vitro. Target: Microtubule/Tubulinin vitro: Maytansinol disrupts the mitotic spindle andprevents mitotic exit in Drosophila. Maytansinol reduces thegrowth and/or survival of HCT116 cells in a dose-dependent…

Bioactivity: MC-DOXHZN is an albumin-binding prodrug of Doxorubicin, withacid-sensitive properties .[1]

Bioactivity: MC-DOXHZN hydrochloride is an albumin-binding prodrug ofDoxorubicin, with acid-sensitive properties .[1]

Bioactivity: Mertansine (DM1) is a inhibitor and is anmicrotubulinantibody-conjugatable maytansinoid that is developed toovercome systemic toxicity associated with maytansine and toenhance tumor-specific delivery. Mertansine can be attached toa monoclonal antibody with a linker to create an antibody-drug…

Bioactivity: Methotrexate is a antagonist, with median of 78 nMfolate IC50in assay.in vitro

Bioactivity: Mitomycin C is an antitumor drug and antibiotic that showsextraordinary ability to inhibit . Mitomycin C isDNA synthesisa DNA cross-linking agent, which induces DNA damaging.

Bioactivity: MMAD is a potent inhibitor, is a toxin payload intubulinantibody drug conjugates ( ).ADCs

Bioactivity: MMAF (Monomethylauristatin F) is an antitubulin agent thatinhibit cell division; inhibits H3397 cell growth with an IC50of 105 nM.

Bioactivity: MMAF hydrochloride is an antitubulin agent that inhibit celldivision; inhibits H3397 cell growth with an of 105 nM.IC50


Dxd (Exatecan derivative for ADC) Cat. No.: HY-13631D

Maytansinol (Ansamitocin P-0) Cat. No.: HY-19474

MC-DOXHZN (Doxorubicin(6-maleimidocaproyl)hydrazone) Cat. No.: HY-16261A

MC-DOXHZN hydrochloride (Doxorubicin(6-maleimidocaproyl)hydrazone hydrochloride) Cat. No.: HY-16261B

Mertansine (DM1; Maytansinoid DM1) Cat. No.: HY-19792

Methotrexate (Amethopterin; CL14377; WR19039) Cat. No.: HY-14519

Mitomycin C (Ametycine) Cat. No.: HY-13316

MMAD (Demethyldolastatin 10; Monomethylauristatin D; Monomethyl Dolastatin 10) Cat. No.: HY-15581

MMAF (Monomethylauristatin F) Cat. No.: HY-15579

MMAF Hydrochloride (Monomethylauristatin F Hydrochloride) Cat. No.: HY-15579A

https://www.MedChemExpress.com/Dxd.htmlhttps://www.MedChemExpress.com/Maytansinol.htmlhttps://www.MedChemExpress.com/DOXO-EMCH.htmlhttps://www.MedChemExpress.com/MC-DOXHZN_hydrochloride.htmlhttps://www.MedChemExpress.com/Mertansine.htmlhttps://www.MedChemExpress.com/Methotrexate.htmlhttps://www.MedChemExpress.com/Mitomycin-C.htmlhttps://www.MedChemExpress.com/MMAD.htmlhttps://www.MedChemExpress.com/mmaf.htmlhttps://www.MedChemExpress.com/MMAF-Hydrochloride.html


Purity: >98%Clinical Data: No Development ReportedSize: 1 mg



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Bioactivity: MMAF-Ome belongs to ADC, and inhibits several tumor cell lineswith s of 0.056 nM, 0.166 nM, 0.183 nM, and 0.449 nM forIC50MDAMB435/5T4, MDAMB361DYT2, MDAMB468, and Raji (5T4 ) cell-

lines, respectively.

Bioactivity: Monomethyl auristatin E (MMAE; SGD-1010) is a syntheticderivative of dolastatin 10 and functions as a potent

inhibitor by inhibiting tubulin polymerization.mitoticMMAE is widely used as a cytotoxic component of antibody-drug

to treat several different cancer types.conjugates (ADCs)

Bioactivity: Paclitaxel (Taxol), a naturally occurring antineoplasticagent, stabilizes , resulting intubulin polymerizationarrest at the G2/M phase of the cell cycle and apoptotic celldeath .[1] [2]

Bioactivity: PF-06380101 is a novel cytotoxic Dolastatin 10 analogue; withexcellent potencies in tumor cell proliferation assays anddifferential ADME properties when compared to other syntheticauristatin analogues that are used in the preparation of ADCs.IC50 value: ~0.2 nM(GI50 in BT474, MDA-MB-361-DYT2 and N87…

Bioactivity: PNU-159682, a highly potent metabolite of the anthracyclinenemorubicin with outstanding cytotoxicity, is a potent ADCs

.cytotoxin

Bioactivity: Taltobulin (HTI-286; SPA-110) is an analogue of Hemiasterlin;potent tubulin inhibitor; ADCs cytotoxin. IC50 value: Target:tubulin in vitro: HTI-286 significantly inhibitedproliferation of all three hepatic tumor cell lines (mean IC50= 2 nmol/L +/- 1 nmol/L) in vitro. Interestingly, no decrease…

Bioactivity: Taltobulin hydrochloride is an analogue of Hemiasterlin;potent tubulin inhibitor; ADCs cytotoxin. IC50 value: Target:tubulin in vitro: HTI-286 significantly inhibits proliferationof all three hepatic tumor cell lines (mean IC50 = 2 nmol/L+/- 1 nmol/L). Interestingly, no decrease in viable primary…

Bioactivity: Taltobulin trifluoroacetate (HTI-286; SPA-110) is an analogueof Hemiasterlin; potent tubulin inhibitor; ADCs cytotoxin.IC50 value: Target: tubulin in vitro: HTI-286 significantlyinhibited proliferation of all three hepatic tumor cell lines(mean IC50 = 2 nmol/L +/- 1 nmol/L) in vitro. Interestingly,…

Bioactivity: Tubulysin A(TubA) is a myxobacterial product that can functionas an antiangiogenic agent in many in vitro assays;anti-microtubule, anti-mitotic, an apoptosis inducer,anticancer, anti-angiogenic, and antiproliferative. IC50value: Target: microtubule Tubulysin A is a novel antibiotic,…

MMAF-OMe (Monomethyl auristatin F methyl ester) Cat. No.: HY-79256

Monomethyl auristatin E (MMAE; SGD-1010) Cat. No.: HY-15162

Paclitaxel (Taxol) Cat. No.: HY-B0015

PF-06380101 Cat. No.: HY-12522

PNU-159682 Cat. No.: HY-16700

Taltobulin (HTI-286; SPA-110) Cat. No.: HY-15584

Taltobulin hydrochloride (HTI-286 hydrochloride; SPA-110 hydrochloride) Cat. No.: HY-15584B

Taltobulin trifluoroacetate (HTI-286 trifluoroacetate; SPA-110 trifluoroacetate) Cat. No.: HY-15584A

Tubulysin A (TubA) Cat. No.: HY-15995

https://www.MedChemExpress.com/MMAF-OMe.htmlhttps://www.MedChemExpress.com/Monomethyl-auristatin-E.htmlhttps://www.MedChemExpress.com/Paclitaxel.htmlhttps://www.MedChemExpress.com/PF-06380101.htmlhttps://www.MedChemExpress.com/pnu-159682.htmlhttps://www.MedChemExpress.com/taltobulin.htmlhttps://www.MedChemExpress.com/Taltobulin-hydrochloride.htmlhttps://www.MedChemExpress.com/Taltobulin-trifluoroacetate.htmlhttps://www.MedChemExpress.com/Tubulysin-A.html

ADC LinkerAntibody-drug conjugates linker

Antibody-drug conjugates (ADCs) consist of a desirable monoclonalantibody, an active cytotoxic drug and an appropriate linker. Anappropriate linker between the antibody and the cytotoxic drugprovides a specific bridge, and thus helps the antibody to selectivelydeliver the cytotoxic drug to tumor cells and accurately releases thecytotoxic drug at tumor sites. In addition to conjugation, the linkersmaintain ADCs’ stability during the preparation and storage stages ofthe ADCs and during the systemic circulation period.The ADCs currently undergoing clinical evaluation contain linkers aremostly classified into two categories: cleavable and noncleavable.Cleavable linkers rely on processes inside the cell to liberate the toxin,

such as reduction in the cytoplasm, exposure to acidic conditions in the lysosome, or cleavage by specific proteaseswithin the cell. Noncleavable linkers require proteolytic degradation of the antibody portion of the ADC for release ofthe cytotoxic molecule, which will retain the linker and the amino acid by which it was attached to the antibody.The selection of linker is target dependent, based on the knowledge of the internalization and degradation of theantibody-target antigen complex, and a preclinical and activity comparison of conjugates. Moreover,in vitro in vivothe choice of a linker is also influenced by which cytotoxin is used, as each molecule has different chemical constraints,and frequently the drug structure lends itself to a specific linker.


https://www.MedChemExpress.com/Targets/ADC Linker.html


Purity: 98.68%Clinical Data: No Development ReportedSize: 10 mg, 50 mg, 100 mg, 200 mg

Purity: 99.66%Clinical Data: No Development ReportedSize: 1 g

Purity: 96.13%Clinical Data: No Development ReportedSize: 50 mg, 100 mg

Purity: 98.13%Clinical Data: No Development ReportedSize: 10 mg, 50 mg, 100 mg, 500 mg

Purity: 98.67%Clinical Data: No Development ReportedSize: 50 mg

Purity: >98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Purity: >98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Purity: >98%Clinical Data: No Development ReportedSize: 1 g


Purity: >98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg, 100 mg

ADC Linker Inhibitors & Modulators

Bioactivity: (Ac)Phe-Lys(Alloc)-PABC-PNP is a useful chemical linker inantibody drug conjugates.

Bioactivity: 6-Maleimidohexanoic acid N-hydroxysuccinimide ester(ECMS) is auseful protective group in antibody drug conjugates.

Bioactivity: 6-Quinoxalinecarboxylic acid, 2,3-bis(bromomethyl)- is anuseful linker for antibody-drug-conjugations (ADCs), extractedfrom [Bioorg Chem. 2012 Apr-Jun;41-42:1-5.] compound 1i.

Bioactivity: DC1, an analogue of the minor groove-binding DNA alkylatorCC-1065, is an antibody conjugate of cytotoxic DNA alkylatorsfor the targeted treatment of cancer.

Bioactivity: DC1-Sme is an antibody conjugate of phosphate prodrug ofcytotoxic DNA alkylators for the targeted treatment of cancer.

Bioactivity: Fmoc-Phe-Lys(Boc)-PAB-PNP is an linker used in theADCsynthesis of antibody-drug conjugates (ADCs).

Bioactivity: Fmoc-Val-Cit-PAB is a linker for antibody-drug-conjugation(ADC).

Bioactivity: Fmoc-Val-Cit-PAB-PNP is a peptide prodrug linker, is a linkerfor antibody-drug-conjugation (ADC).

Bioactivity: MC-Val-Cit-PAB is a cathepsin cleavable that isADC linkerused for making antibody-drug conjugate. FDA approved drugssuch as brentuximab vedotin use this linker.

Bioactivity: Mc-Val-Cit-PABC-PNP is a cathepsin cleavable usedADC linkerin the synthesis of antibody-drug conjugates (ADCs).

(Ac)Phe-Lys(Alloc)-PABC-PNP Cat. No.: HY-20560

6-Maleimidohexanoic acid N-hydroxysuccinimide ester (EMCS) Cat. No.: HY-78961

6-Quinoxalinecarboxylic acid, 2,3-bis(bromomethyl)- Cat. No.: HY-21210

DC1 Cat. No.: HY-112899

DC1-SMe Cat. No.: HY-112898

Fmoc-Phe-Lys(Boc)-PAB-PNP Cat. No.: HY-114430

Fmoc-Val-Cit-PAB Cat. No.: HY-19318

Fmoc-Val-Cit-PAB-PNP Cat. No.: HY-41189

MC-Val-Cit-PAB Cat. No.: HY-78738

Mc-Val-Cit-PABC-PNPCat. No.: HY-20336

https://www.MedChemExpress.com/Targets/ADC Linker.htmlhttps://www.MedChemExpress.com/_ac_phe-lys_alloc_-pabc-pnp.htmlhttps://www.MedChemExpress.com/6-maleimidohexanoic-acid-n-hydroxysuccinimide-ester.htmlhttps://www.MedChemExpress.com/6-Quinoxalinecarboxylic-acid,-2,3-bis_bromomethyl_-.htmlhttps://www.MedChemExpress.com/DC1.htmlhttps://www.MedChemExpress.com/DC1-SMe.htmlhttps://www.MedChemExpress.com/Fmoc-Phe-Lys_Boc_-PAB-PNP.htmlhttps://www.MedChemExpress.com/Fmoc-Val-Cit-PAB.htmlhttps://www.MedChemExpress.com/Fmoc-Val-Cit-PAB-PNP.htmlhttps://www.MedChemExpress.com/MC-Val-Cit-PAB.htmlhttps://www.MedChemExpress.com/Mc-Val-Cit-PABC-PNP.html

Purity: 99.64%Clinical Data: No Development ReportedSize: 100 mg, 500 mg, 1 g


Bioactivity: UAA crosslinker 1 act as substrates for pylRS/tRNA pair thatenable its incorporation into a target protein.

Bioactivity: Val-cit-PAB-OH is a peptide prodrug linker.


UAA crosslinker 1 Cat. No.: HY-111434

Val-cit-PAB-OH Cat. No.: HY-12362

https://www.MedChemExpress.com/UAA_crosslinker_1.htmlhttps://www.MedChemExpress.com/Val-cit-PAB-OH.html


Drug-Linker Conjugates for ADC

Drug-Linker Conjugates for Antibody Drug Conjugates (ADC)comprise of an active cytotoxic drug and an appropriate linker. TheDrug-Linker Conjugates can expand the utility of monoclonalantibody (mAbs) and improve their potency and effectiveness. Thesite-specific conjugations of Drug-Linker to an antibody may involvegenetic engineering of the mAb to introduce discrete, availablecysteines or non-natural amino acids with an orthogonally-reactivefunctional group handle. These site-specific approaches not onlyincrease the homogeneity of ADCs but also enable novelbio-orthogonal chemistries that utilize reactive moieties other thanthiol or amine. The cytotoxic drug, monomethyl auristatin E (MMAE),

is conjugated to the three trastuzumab variants using a protease cleavable linker and shows in vivo therapeuticefficacy.

https://www.MedChemExpress.com/Targets/Antibody-drug Conjugate.html


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Purity: >98%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

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Purity: >98%Clinical Data: No Development ReportedSize: 1 mg




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Drug-Linker Conjugates for ADC Inhibitors & Modulators

Bioactivity: Acetylene-linker-Val-Cit-PABC-MMAE consists the ADCs linker(Acetylene-linker-Val-Cit-PABC) and potent tubulin inhibitor(MMAE), Acetylene-linker-Val-Cit-PABC-MMAE is an antibody drugconjugate.

Bioactivity: AcLys-PABC-VC-Aur0101 is a cleavable anti-CXCR4 drug-linker.conjugates for ADC

Bioactivity: AmPEG6C2-Aur0131 is a non-cleavable anti-CXCR4 drug-linker.conjugates for ADC

Bioactivity: Monomethyl auristatin D (MMAD), a potent tubulin inhibitor, isa toxin payload in antibody drug conjugate. IC50 Value: N/ATarget: tubulin; ADCs For comparison purposes, the ADC A1-mc-MMAD and/or A1 -vc-MMAD were used. The linker payload,mc-MMAD (6-maleimidocaproyl-monomethylauristatin-D) was…

Bioactivity: DBCO-(PEG)3-VC-PAB-MMAE is made by MMAE conjugated toDBCO-(PEG)3-vc-PAB linker. Monomethyl auristatin E (MMAE), apotent tubulin inhibitor, is a toxin payload in antibody drugconjugate.

Bioactivity: Deruxtecan, a toxin and linker moiety of DS-8201, is adrug-linker conjugate for antibody-drug conjugate (ADC)extracted from patent WO2017002776A1, compound 1.

Bioactivity: Fmoc-Val-Cit-PAB-MMAE consists the ADCs linker(Fmoc-Val-Cit-PAB) and potent tubulin inhibitor (MMAE),Fmoc-Val-Cit-PAB-MMAE is an antibody drug conjugate.

Bioactivity: MAL-di-EG-Val-Cit-PAB-MMAE consists the ADCs linker(MAL-di-EG-Val-Cit-PAB) and potent inhibitor (MMAE),tubulinMAL-di-EG-Val-Cit-PAB-MMAE is an antibody drug conjugate.

Bioactivity: Monomethyl auristatin D (MMAD), a potent tubulin inhibitor, isa toxin payload in antibody drug conjugate; Mc-MMAD is aprotective group (maleimidocaproyl) -conjugated MMAD. IC50Value: Target: tubulin; ADCs For comparison purposes, the ADCA1 -mc-MMAD and/or A1 -vc-MMAD were used. The linkerpayload,…

Bioactivity: Mc-MMAE is a protective group (maleimidocaproyl)-conjugatedmonomethyl auristatin E (MMAE), which is a potent tubulininhibitor, is a toxin payload in antibody drug conjugate (

).ADC


Acetylene-linker-Val-Cit-PABC-MMAE (LCB14-0602) Cat. No.: HY-19812

AcLys-PABC-VC-Aur0101 Cat. No.: HY-111554

AmPEG6C2-Aur0131 Cat. No.: HY-111555

Cys-mcMMAD Cat. No.: HY-15750

DBCO-(PEG)3-VC-PAB-MMAE Cat. No.: HY-111012

Deruxtecan Cat. No.: HY-13631E

Fmoc-Val-Cit-PAB-MMAE Cat. No.: HY-19811

MAL-di-EG-Val-Cit-PAB-MMAE Cat. No.: HY-100567

Mc-MMAD Cat. No.: HY-15740

Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) Cat. No.: HY-15741

https://www.MedChemExpress.com/Targets/Drug-Linker Conjugates for ADC.htmlhttps://www.MedChemExpress.com/Acetylene-linker-Val-Cit-PABC-MMAE.htmlhttps://www.MedChemExpress.com/AcLys-PABC-VC-Aur0101.htmlhttps://www.MedChemExpress.com/AmPEG6C2-Aur0131.htmlhttps://www.MedChemExpress.com/cys-mcmmad.htmlhttps://www.MedChemExpress.com/DBCO-_PEG_3-VC-PAB-MMAE.htmlhttps://www.MedChemExpress.com/Deruxtecan_analog.htmlhttps://www.MedChemExpress.com/Fmoc-Val-Cit-PAB-MMAE.htmlhttps://www.MedChemExpress.com/MAL-di-EG-Val-Cit-PAB-MMAE.htmlhttps://www.MedChemExpress.com/Mc-MMAD.htmlhttps://www.MedChemExpress.com/Mc-MMAE.html






1 mg, 5 mg, 10 mg


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




1 mg, 5 mg, 10 mg



1 mg, 5 mg, 10 mg

Bioactivity: Mc-MMAF is a protective group-conjugated MMAF. MMAF is a morepotent drug than Monomethyl auristatin E (MMAE), but ischarged and relatively membrane-impermeable, is a potenttubulin inhibitor, is a toxin payload in antibody drugconjugate. Target: MMAF is a new auristatin derivative with a…

Bioactivity: mDPR-Val-Cit-PAB-MMAE consists the ADCs linker(mDPR-Val-Cit-PAB) and potent tubulin inhibitor (MMAE),mDPR-Val-Cit-PAB-MMAE is an antibody drug conjugate.

Bioactivity: N3-PEG3-vc-PAB-MMAE is a withdrug-linker conjugate for ADCpotent antitumor activity by using the anti-mitotic agent,monomethyl auristatin E (MMAE), linked via the peptideN3-PEG3-vc-PAB.

Bioactivity: NAMPT inhibitor-linker 1 is a drug-linker conjugates for ,ADCcomposed of an inhibitor as a payload, and a linker.NAMPTADC-3 consists of an NAMPT inhibitor-linker 1 and ananti-c-Kit monoclonal antibody, exihibits potent activityagainst c-Kit expressing cell lines such as GIST-T1 and…

Bioactivity: NAMPT inhibitor-linker 2 is a drug-linker conjugates for ,ADCcomposed of an inhibitor as a payload, and a linker.NAMPTADC-4 consists of an NAMPT inhibitor-linker 2 and ananti-c-Kit monoclonal antibody, exihibits potent activityagainst c-Kit expressing cell lines such as GIST-T1 and…

Bioactivity: SMCC-DM1 is DM1 with a reactive linker SMCC to make antibodydrug conjugate. DM1 (mertansine), a thiol-containingmaytansinoid, is a potent microtubule-disrupting agent.

Bioactivity: SPDB-DM4 is a by using thedrug-linker conjugate for ADCmaytansinebased payload (DM4) via a SPDB linker, exhibitingpotent anti-tumor activity.

Bioactivity: ST8154AA1 is a part of antibody drug conjugates ( )ADCscharged with inhibitor by a linker, shows antitumorHDACactivity .[1]

Bioactivity: ST8155AA1 is a part of antibody drug conjugates ( )ADCscharged with inhibitor by a linker, shows antitumorHDACactivity .[1]

Bioactivity: sulfo-SPDB-DM4 is a by using thedrug-linker conjugate for ADCmaytansinebased payload (DM4) via the sulfo-SPDB linker.

McMMAF (Maleimidocaproyl monomethylauristatin F) Cat. No.: HY-15578

mDPR-Val-Cit-PAB-MMAE Cat. No.: HY-19813

N3-PEG3-vc-PAB-MMAE Cat. No.: HY-100874

NAMPT inhibitor-linker 1 Cat. No.: HY-112615

NAMPT inhibitor-linker 2 Cat. No.: HY-112616

SMCC-DM1 (DM1-SMCC) Cat. No.: HY-101070

SPDB-DM4 Cat. No.: HY-12460

ST8154AA1 Cat. No.: HY-112805

ST8155AA1 Cat. No.: HY-112806

sulfo-SPDB-DM4 Cat. No.: HY-101141

https://www.MedChemExpress.com/McMMAF.htmlhttps://www.MedChemExpress.com/mDPR-Val-Cit-PAB-MMAE.htmlhttps://www.MedChemExpress.com/N3-PEG3-vc-PAB-MMAE.htmlhttps://www.MedChemExpress.com/NAMPT_inhibitor-linker_1.htmlhttps://www.MedChemExpress.com/NAMPT_inhibitor-linker_2.htmlhttps://www.MedChemExpress.com/SMCC-DM1.htmlhttps://www.MedChemExpress.com/SPDB-DM4.htmlhttps://www.MedChemExpress.com/st8154aa1.htmlhttps://www.MedChemExpress.com/st8155aa1.htmlhttps://www.MedChemExpress.com/sulfo-SPDB-DM4.html


1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Purity: >98%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

1 mg, 5 mg, 10 mg


1 mg, 5 mg, 10 mg



1 mg, 5 mg, 10 mg

Bioactivity: SuO-Val-Cit-PAB-MMAE is a bydrug-linker conjugate for ADCusing the anti-mitotic agent, monomethyl auristatin E (MMAE),linked via the peptide SuO-Val-Cit-PAB.

Bioactivity: SW-163D-AcLysValCit-PABC-DMAE is a Drug-Linker Conjugates for which consists of a natural bis-intercalator, SW-163D,ADC

conjugated via an AcLysValCitPABC-DMAE linker .[1]

Bioactivity: Val-Cit-PAB-MMAE is a by usingdrug-linker conjugate for ADCthe anti-mitotic agent, monomethyl auristatin E (MMAE), linkedvia the peptide Val-Cit-PAB.

Bioactivity: Vc-MMAD consists the ADCs linker(Val-Cit) and potent tubulininhibitor (MMAD), Vc-MMAD is an antibody drug conjugate. IC50Valu: N/A Target: tubulin; ADCs Monomethyl auristatin D(MMAD), a potent tubulin inhibitor, is a toxin payload andantibody drug conjugate. For comparison purposes, the ADC A1…

Bioactivity: VcMMAE is a with potentdrug-linker conjugate for ADCantitumor activity by using the anti-mitotic agent, monomethylauristatin E (MMAE), linked via the lysosomally cleavabledipeptide, valine-citrulline (vc).


SuO-Val-Cit-PAB-MMAE Cat. No.: HY-100566

SW-163D-AcLysValCit-PABC-DMAE Cat. No.: HY-114325

Val-Cit-PAB-MMAE Cat. No.: HY-100374

Vc-MMAD Cat. No.: HY-15742

VcMMAE (mc-vc-PAB-MMAE) Cat. No.: HY-15575

https://www.MedChemExpress.com/SuO-Val-Cit-PAB-MMAE.htmlhttps://www.MedChemExpress.com/SW-163D-AcLysValCit-PABC-DMAE.htmlhttps://www.MedChemExpress.com/Val-Cit-PAB-MMAE.htmlhttps://www.MedChemExpress.com/Vc-MMAD.htmlhttps://www.MedChemExpress.com/VcMMAE.html


PROTAC-linker Conjugate for PACPROTAC-linker for PROTAC-antibody Conjugate

PROTAC-linker Conjugate for PAC comprises an antibody conjugatedvia a linker to a PROTAC. The PROTAC-Antibody Conjugate (PAC)molecules comprise an antibody conjugated via a linker (L1) to aPROTAC, wherein the PROTAC comprises an ubiquitin E3 ligasebinding groug (“E3LB”), a linker (“L2”) and a protein binding group(“PB”). To obtain a PAC having potent efficacy and a desirabletherapeutic index, the following components are provided. 1.Antibody (Ab): The antibody portion of a PAC can target a cell thatexpresses an antigen whereby the antigen specific PAC is deliveredintracellularly to the target cell, typically through endocytosis WhilePACs that comprise an antibody directed to an antigen that is not

found on the cell surface may result in less specific intracellular delivery of the PROTAC portion into the cell, the PACmay still undergo pinocytosis. 2. Linkers (L1): A“linker” (L1) is a bifunctional or multifunctional moiety that can be usedto link one or more PROTAC moieties (D) to an antibody (Ab) to form a PAC. In some embodiments, PACs can beprepared using a L1 having reactive functionalities for covalently attaching to the PROTAC and to the antibody. 3.PROTAC(D).

https://www.MedChemExpress.com/Targets/PROTAC-linker Conjugate for PAC.html


PROTAC-linker Conjugate for PAC Inhibitors & Modulators

Bioactivity: PAC comprises an antibody conjugated via a linker to a. PAC extracts from patent WO2017201449A1, compoundPROTAC

LP2. PAC is a more marked ( )estrogen receptor-alpha ERαdegrader compared to PROTAC (without Ab).


PAC Cat. No.: HY-112100
https://www.MedChemExpress.com/Targets/PROTAC-linker Conjugate for PAC.htmlhttps://www.MedChemExpress.com/PAC.html

Antibody-drug Conjugate/ADC Related...Antibody-drug conjugates. Bioactivity: Auristatin F is a...

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