A highly potent, orally bioavailable, pan-VEGFR inibitor with IC50 of 1, 5, 3 nM for VEGFR1, 2, 3, respectively; also inhibits c-Kit and PDGFRβ with IC50 of 2 and 5 nM, >36-fold selectivity over PDGFR-α, >1000-fold over Flt-3 and EGFR; inhibits VEGF-stimulated proliferation and KDR phosphorylation with IC50 of 0.4 and 0.5 nM in human umbilical vein endothelial cells; inhibits angiogenesis, neovascular survival and tumor growth in vivo.
