Description
A dual VEGFR and PDGFR family kinase inhibitor (IC50s = 0.003, 0.004, 0.004, 0.19, 0.066, 0.003, and 0.014 µM for VEGFR1, VEGFR2, FLT3, VEGFR3, PDGFRβ, CSF-1R, and KIT, respectively); is selective for these kinases over RET, FGFR, Src, EGFR, and c-Met (IC50s = 1.9, >12.5, >50, >50, and >50 µM, respectively); inhibits Tie2 (IC50 = 0.17 µM); inhibits the proliferation of HT-29, MDA-MB-435, 9L, and MV4-11 cells (IC50s = 1.3, 2.4, 0.27, and 0.004 µM, respectively); induces apoptosis in MV4-11 cells (IC50 = 0.03 µM); inhibits VEGF-induced uterine edema in mice (ED50 = 0.5 mg/kg); improves survival in a MOLM-13 leukemia mouse xenograft model at 1, 3, and 10 mg/kg