Sorafenib Tosylate...2 | Applications: At a concentration of 100 nM, Sorafenib induced 43.6 ± 5.2%...
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1 | www.apexbt.com Sorafenib Tosylate Cat. No.: A8245 CAS No.: 475207-59-1 Formula: C21H16ClF3N4O3·C7H8O3S M.Wt: 637.03 Synonyms: Target: Tyrosine Kinase Pathway: PDGFR Storage: Store at -20°C In Vitro ı31.85mg/mL in DMSO, ı4.15 mg/mL in EtOH with ultrasonic,insoluble in H2O Preparing Stock Solutions Mass 1mg 5mg 10mg Solvent Concentration 1 mM 1.5698 mL 7.8489 mL 15.6978 mL 5 mM 0.3140 mL 1.5698 mL 3.1396 mL 10 mM 0.1570 mL 0.7849 mL 1.5698 mL Please refer to the solubility information to select the appropriate solvent. Shortsummary Raf kinases and tyrosine kinases inhibitor IC₅₀ & Target 6 nM (Raf-1), 22 nM (B-Raf), 90 nM (VEGFR2), 57 nM (PDGFRβ) In Vitro Cell Viability Assay Cell Line: MV4-11 and EOL-1 cells Preparation method˖ The solubility of this compound in DMSO is > 31.9 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. Reacting conditions: 100 pM ~ 10 μM; 72 hrs for MV4-11 cells and 24 hrs for EOL-1 cells Product Name: Sorafenib Tosylate Revision Date: 01/10/2020 Product Data Sheet Solvent & Solubility Biological Activity 1 | www.apexbt.com Sorafenib Tosy l l l l l l l l l l l la a a a a a a a a a at t t t t t t t t t t te e e e e e e e e e e e Cat. No.: A824 4 4 4 4 4 4 4 4 5 5 5 5 5 5 5 5 5 5 5 CAS No.: 47 47 47 7 7 7 7 7 4 4 47 47 47 47 47 47 47 47 4 52 52 52 52 52 52 52 52 52 5207 07 07 07 07 07 07 07 07 07 7 07 7 - - - - - - 59 5 5 5 5 5 5 5 5 5 5 5 - 1 Formula: C2 C C2 C2 C2 C2 C C C2 C2 C2 C2 C2 C C21H16ClF3N4O3·C7H8O3S S M.Wt: 637.03 Synonyms: T arget: Tyrosine Kinase Pathway: PDGFR Storage: Store at - 20°C In Vitro ı 31.85mg/mL in DMSO, ı 4.15 mg/mL in EtOH with ultrasonic,insol ol ol ol ol ol ol ol ol l l l lub ub ub ub ub ub ub ub ub ub ub u ub ble in H2O Preparing Stock Solutions Mass 1mg 5mg 10mg Solvent Concentration 1 mM 1.5698 mL 7.8489 mL 15.6978 mL 5 mM 0.3140 mL 1.5698 8 8 m m m m m m m m m mL L L L L L L L L 3.1396 mL 1 0 mM 0.1570 mL 0. 0. 0. 0. 0 0. 0. 0. 0. 0. 0 78 8 8 78 8 78 78 78 78 78 78 78 78 78 78 8 7 49 49 49 49 49 49 49 49 49 49 4 4 4 4 4 4 m m m m m m m m m m m m mL L L L L L L L L L L 1.5698 mL Pl Pl Pl Pl Pl Pl Pl Pl P Pl P ea ea ea ea ea ea ea ea ea ea ea ease se se se se se se se se se e r r r r r r r r r r r r r r r ref ef ef ef ef ef ef ef ef ef ef f f fer e e e e e e e e e e to the solubility information to select the appropriate solve ve ve e e e e e e ent nt nt nt nt nt nt nt nt t n . . Shortsummary Raf kinases and tyrosine kinases inhibitor IC ₅₀ & Target 6 nM (Raf - 1), 22 nM (B - Raf), 90 nM (VEGFR2), 57 nM (PDGFRβ) In Vitro Cell Viabili i i i i ity ty ty ty y ty ty ty ty ty ty y A A A A A A A A A A As s s ss s s s s s s ay Cell L L L L L L L L L Lin in in in i i i in in n n n n n ne: e: e: e: e e: e: e: e MV4 - 11 and EOL - 1 cells Pr Pr Pr Pr Pr Pr Pr Pr Pr r P ep ep ep ep ep ep ep ep ep ep ar ar ar ar ar ar ar ar ar ar ar r ar at at at at at at at a at at at a a i i io i i i n method ˖ The solubility of this compound in n n n n n n n n n n n n n D D D D D D D D D D D D D D DMS MS MS MS MS MS MS MS MS MS MS S S MS S S S MS S S MS S S S MSO O O O O O O O O O O O O O is > 31.9 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. Reacting conditions: 100 pM ~ 10 μM; 72 hrs for MV4 - 11 cells and 24 hrs for EOL - 1 cells Product Name : Sorafenib Tosylate Revision Date: 0 1 / 1 0 / 0 20 20 et Product Data Shee Solvent & So o o o o ol l l l l lu u u u ub b b b bi i i i i il l l l li i i i i i i i it t t t t t ty y y y y Biological Activity
Transcript of Sorafenib Tosylate...2 | Applications: At a concentration of 100 nM, Sorafenib induced 43.6 ± 5.2%...
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1 | www.apexbt.com
Sorafenib TosylateCat. No.: A8245
CAS No.: 475207-59-1
Formula: C21H16ClF3N4O3·C7H8O3S
M.Wt: 637.03
Synonyms:
Target: Tyrosine Kinase
Pathway: PDGFR
Storage: Store at -20°C
In Vitro
31.85mg/mL in DMSO, 4.15 mg/mL in EtOH with ultrasonic,insoluble in H2O
Preparing
Stock Solutions
Mass
1mg 5mg 10mgSolvent
Concentration
1 mM 1.5698 mL 7.8489 mL 15.6978 mL
5 mM 0.3140 mL 1.5698 mL 3.1396 mL
10 mM 0.1570 mL 0.7849 mL 1.5698 mL
Please refer to the solubility information to select the appropriate solvent.
Shortsummary Raf kinases and tyrosine kinases inhibitor
IC₅₀ & Target 6 nM (Raf-1), 22 nM (B-Raf), 90 nM (VEGFR2), 57 nM (PDGFRβ)
In Vitro
Cell Viability Assay
Cell Line: MV4-11 and EOL-1 cells
Preparation method The solubility of this compound in DMSO is > 31.9 mg/mL. General tips for
obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes
and/or shake it in the ultrasonic bath for a while. Stock solution can be stored
below - 20 °C for several months.
Reacting conditions: 100 pM ~ 10 μM; 72 hrs for MV4-11 cells and 24 hrs for EOL-1 cells
Product Name: Sorafenib TosylateRevision Date: 01/10/2020
Product Data Sheet
Solvent & Solubility
Biological Activity
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Sorafenib TosyyyyyyyyyyyllllllllllllaaaaaaaaaaatttttttttttteeeeeeeeeeeeCat. No.: A82444444444455555555555
CAS No.: 474747777774447474747474747474 525252525252525252520707070700707070707077077------5955555555555 -1
Formula: C2CC2C2C2C2CCC2C2C2C2C2CC21H16ClF3N4O3·C7H8O3SS
M.Wt: 637.03
Synonyms:
Target: Tyrosine Kinase
Pathway: PDGFR
Storage: Store at -20°C
In Vitro
31.85mg/mL in DMSO, 4.15 mg/mL in EtOH with ultrasonic,insolololololololololllllubububububububububububuubble in H2O
Preparing
Stock Solutions
Mass
1mg 5mg 10mgSolvent
Concentration
1 mM 1.5698 mL 7.8489 mL 15.6978 mL
5 mM 0.3140 mL 1.569888888 mmmmmmmmmmLLLLLLLLL 3.1396 mL
10 mM 0.1570 mL 0.0.0.0.00.0.0.0.0.0 78887887878787878787878787887 49494949494949494949444444 mmmmmmmmmmmmmLLLLLLLLLLL 1.5698 mL
PlPlPlPlPlPlPlPlPPlP eaeaeaeaeaeaeaeaeaeaeaeasesesesesesesesesesee rrrrrrrrrrrrrrrrefefefefefefefefefefeffffereeeeeeeeee to the solubility information to select the appropriate solveveveeeeeeeentntntntntntntntnttn ..
Shortsummary Raf kinases and tyrosine kinases inhibitor
IC₅₀ & Target 6 nM (Raf-1), 22 nM (B-Raf), 90 nM (VEGFR2), 57 nM (PDGFRβ)
In Vitro
Cell Viabiliiiiiitytytytyytytytytytytyy AAAAAAAAAAAsssssssssss ay
Cell LLLLLLLLLLininininiiiininnnnnnne:e:e:e:ee:e:e:e MV4-11 and EOL-1 cells
PrPrPrPrPrPrPrPrPrrP epepepepepepepepepepparararararararararararrarratatatatatatataatatataa iiioiii n method The solubility of this compound innnnnnnnnnnnnn DDDDDDDDDDDDDDDMSMSMSMSMSMSMSMSMSMSMSSSMSSSSMSSSMSSSSMSOOOO OOOOOOOOOO is > 31.9 mg/mL. General tips for
obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes
and/or shake it in the ultrasonic bath for a while. Stock solution can be stored
below - 20 °C for several months.
Reacting conditions: 100 pM ~ 10 μM; 72 hrs for MV4-11 cells and 24 hrs for EOL-1 cells
Product Name: Sorafenib TosylateyRevision Date: 01/10/ 02020
etProduct Data Shee
Solvent & Soooooolllllluuuuubbbbbiiiiiillllliiiiiiiiitttttttyyyyy
Biological Activity
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Applications: At a concentration of 100 nM, Sorafenib induced 43.6 ± 5.2% of the cells to
undergo apoptosis. In EOL-1 cells, Sorafenib at a concentration as low as 10
nM promoted 89.29 ± 1.8% of the cells to undergo apoptosis. In addition, cell
cycle analysis of Sorafenib-treated MV4-11 cells showed that Sorafenib
dose-dependently induced cell cycle arrest with an increase in the percentages
of cells in G0/G1 from 52.7 ± 0.9% (the control group) to 66.8 ± 1.5% (the 100
nM Sorafenib group).
In Vivo
Animal experiment
Animal models: Athymic mice bearing FLT3-ITD tumors
Dosage form: 0.3, 1.0, 3 or 10 mg/kg; p.o.
Applications: In athymic mice bearing FLT3-ITD tumors, Sorafenib showed dose-dependent
antitumor activity. At the doses of 3 and 10 mg/kg, 6 and 9 out of 10 mice
showed complete responses, respectively. According to the Western blot
analysis of MV4-11 tumors, phosphorylation of STAT5 was completely
abolished 3 hrs after the second administration. Meanwhile, phospho-histone
H3 was also significantly reduced.
Other notes: Please test the solubility of all compounds indoor, and the actual solubility may
slightly differ with the theoretical value. This is caused by an experimental
system error and it is normal.
1. Ming-Hua Hsu, Shih-Ming Hsu, et al. "Treatment with low-dose sorafenib in combination with a novel benzimidazole derivative
bearing a pyrolidine side chain provides synergistic anti-proliferative effects against human liver cancer." RSC Adv., 2017, 7,
16253-16263.
See more customer validations on www.apexbt.com.
[1]. D Auclair, D Miller, V Yatsula, et al. Antitumor activity of sorafenib in FLT3-driven leukemic cells. Leukemia, 2007, 21:439-445.
FOR RESEARCH PURPOSES ONLY.NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.Specific storage and handling information for each product is indicated on the product datasheet. Most APExBIO products are stable
under the recommended conditions. Products are sometimes shipped at a temperature that differs from the recommended storage
temperature. Shortterm storage of many products are stable in the short-term at temperatures that differ from that required for
long-term storage. We ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt
of the product, follow the storage recommendations on the product data sheet.
Product Citations
References
Caution
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Applications: At a concentration of 100 nM, Sorafenib induced 43.6 ± 5.2% of the cells to
undergo apoptosis. In EOL-1 cells, Sorafenib at a concentration as low as 10
nM promoted 89.29 ± 1.8% of the cells to undergo apoptosis. In addition, cell
cycle analysis of Sorafenib-treated MV4-11 cells showed that Sorafenib
dose-dependently induced cell cycle arrest with an increase in the percentages
of cells in G0/G1 from 52.7 ± 0.9% (the control grrrrrrrrrrououououououououoouoo p)p)p)p)p)p)p)p)p)p)p) tttttttttto o o oo o oooo o 666666666666666666666666666 .8 ± 1.5% (the 100
nM Sorafenib group).
In Vivo
AnAnAnAnAnAnAnAnAnnAAAAAAAA imimimimimmimimimimmalalalalalalalalalalalaal eeexe periment
AAAAAAAAAnAAAAAA imal models: Athymic mice bearing FLT3-ITD tumomomomomomommomomomoomomooorsrsrsrsrsrsrsrsrsrsrsrsrsr
Dosage form: 0.3, 1.0, 3 or 10 mg/kg; p.o.
Applications: In athymic mice bearing FLT3-ITD tumors, Sorafenib showed dose-dependent
antitumor activity. At the doses of 3 and 10 mg/kg, 6 and 9 out of 10 mice
showed complete responses, respectively. According to the Western blot
analysis of MV4-11 tumors, phosphorylation of STAT5 was completely
abolished 3 hrs after the second administration. Meanwwwwwwwwhihihihihhihihhhihh leleleleleleeleleleee, phospho-histone
H3 was also significantly reduced.
OtOtOtOtOtOtOtOOtOtOOthehehehehehehehehehherrrrrrr r rrr nonononononononoonononootetetetetetetettetetetes: Please test the solubility of all compounds inininininininindodododododododododooororororoororororor,,,,,,,, ananananananananannananndddddddddddd the actual solubility may
slightly differ with the theoretical vaaaaaaaaaaaaluluulululululululululuuuluue.e.e.e.e.e.e.ee.e.e.e.e.e. TTTTTTTTTTTTTTTTTTTThihihihihihihihihihihhih s ss s s ss ssss s isiiiiii caused by an experimental
system error and it is normal.
1. Ming-Hua Hsu, Shih-Ming Hsu, et al. "Treatment with low-dose sorafenib in combination with a novel benzimidazole derivative
bearing a pyrolidine side chain provides synergistic anti-proliferative effects against human liver cancer." RSC Adv., 2017, 7,
16253-16263.
See more customer validaaaaaaaaaatitittititittitititt ononoonononononononononoo sssssssssss oooooonooooooo www.apexbt.com.
[1]. D Auclair, D Miller, V Yatsula, et al. Antitumor activity of sorafenib in FLT3-driven leukemic cells. Leukemia, 2007, 21:439-445.
FOR RESEARCH PURPOSES S S SS ONONONONONONONONONONONNLYLYLYLYLYLYLYLLYLYLYY..........NOT FOR HUMAN, VETTERERERERERERERERERERREERINININININNNNININNNINNININNI ARARARARARARARARARARARARRARARARRRARRY YY Y Y Y YY YYYY DDDDDDDIDDD AGNOSTIC OR THERAPEUTTIC USE.Specific storage and hhhhhhhhhanananananannaaanaa dldldldldldldldldldldlddlinininininininininng g g g ggg g ggg ggg iniininiiniiininformation for each product is indicatted on the product datatatatatatatatattatatatasasasasasasassasaasasassasssaaashehehehehehehehehehehhehehehh etetetetetetettetetett. Most APExBEE IO ble products are stab
under the recommmmmmmmmmmmmmmmenenenenenenennnenenenennnndededdedededeeeeeeddeeddededdeeeedded ddddd ddddddddddd conditions. Products are sometimes shipped at a te erature that differs from the recommended stor eed at a temperature that differs from the recommended storag
temperature. Shortterm storage of many products are stable in the sshort-term at temperatures that differ from that required for
long-term storage. We ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt e
of the product, follow the storage recommendations on the product ddata sheet.
Product Citations
Referrrrrreeeeeeennnnnnncccccccccceeees
Caution
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7505 Fannin street, Suite 410, Houston, TX 77054. Tel: +1-832-696-8203 | Fax: +1-832-641-3177 | Email: [email protected]
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