Description
A multi-kinase inhibitor that inhibits VEGFR2, VEGFR3, VEGFR1, EGFR, PDGFRβ, Tie-2, and FGFR1 (IC50s = 40, 110, 1,600, 500, 1,100, 2,500, and 3,600 nM, respectively, in cell-free assays); also binds to 142 additional kinases in a panel of 442 kinases (Kds = 4.6-7,900 nM); induces apoptosis and cell cycle arrest at the G0/G1 phase in GEO colon and OVCAR-3 ovarian cancer cells at 1 and 2.5 µM; inhibits proliferation of HAK1-B, KYN-2, and Huh7 hepatocarcinoma cells and HUVECs (IC50s = 10, 8.1, 9.4, and 7.1 µM, respectively); increases survival and decreases tumor angiogenesis and VEGFR2 levels in a D54MG glioblastoma mouse xenograft model at 200 mg/kg; reduces tumor growth in a variety of mouse xenograft models at 25-100 mg/kg per day