Sitravatinib

A novel, broad spectrum small molecule inhibitor that blocks a wide array of RTKs known to be amplified/overexpressed in sarcomas, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl (IC50=1.5-30 nM) ; significantly blocks the phosphorylation of potential driver RTKs and induces potent anti-proliferative effects in vitro; suppresses tumor growth in tumor xenografts in vivo.Lung Cancer Phase 2 Clinical (In Vitro) :Sitravatinib (0.01 nM-10 μM; 14 days) reduces colony formation in a dose-dependent manner in KLN205 and E0771 cell lines.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. (In Vivo) :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.