Sitravatinib malate (MGCD516 malate) is an orally bioavailablereceptor tyrosine kinase (RTK)inhibitor withIC₅₀s 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^[1]. Sitravatinib malate shows potent single-agent antitumor efficacy and enhances the activity ofPD-1blockade through promoting an antitumor immune microenvironment^[2].

Sitravatinib (0.01 nM-10 μM; 14 days) reduces colony formation in a dose-dependent manner in KLN205 and E0771 cell lines^[2].
Sitravatinib (0.001-10 μM; 5 days) inhibits tumor cell viability with IC₅₀s of approximately 1 μM in KLN205, E0771 and CT1B-A5 cell lines^[2].

Sitravatinib (20 mg/kg; p.o.; once per day for 6 days) significantly inhibits tumor progression and induces tumor regression in C57BL/6 mice bearing CT1B-A5 cells model^[2].

763.76

C₃₇H₃₅F₂N₅O₉S

2244864-88-6

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