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Sitravatinib malate

Sitravatinib malate
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Sitravatinib malate

Catalog No. T12925Cas No. 2244864-88-6
Sitravatinib malate is an orally bioavailable receptor inhibitor of tyrosine kinase (RTK) (IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively.) , shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
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Pack SizePriceAvailabilityQuantity
25 mg$1,5201-2 weeks
50 mg$1,9801-2 weeks
100 mg$2,5001-2 weeks
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Product Introduction

Bioactivity
Description
Sitravatinib malate is an orally bioavailable receptor inhibitor of tyrosine kinase (RTK) (IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively.) , shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
Targets&IC50
DDR2:0.5 nM, c-Kit:6 nM, DDR1:29 nM, VEGFR1:6 nM, Mer:2 nM, Axl:1.5 nM, VEGFR3:2 nM, VEGFR2:5 nM, TrkB:9 nM, FLT3:8 nM, TrkA:5 nM
In vitro
In KLN205 and E0771 cell lines,Sitravatinib (0.01 nM-10 μM; 14 days) reduces colony formation in a dose-dependent manner [2]. Sitravatinib (0.001-10 μM; 5 days) inhibits tumor cell viability(IC50s : 1 μM, in KLN205), E0771 and CT1B-A5 cell lines[2].
In vivo
In C57BL/6 mice bearing CT1B-A5 cells model,Sitravatinib (20 mg/kg; p.o.; once per day for 6 days) significantly inhibits tumor progression and induces tumor regression [2].
AliasMGCD516 malate, MG-516 malate
Chemical Properties
Molecular Weight763.76
FormulaC37H35F2N5O9S
Cas No.2244864-88-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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