252003-65-9

CP 547,632 is an orally bioavailable and potent inhibitor of the receptor tyrosine kinases VEGF receptor 2 (VEGFR2) and basic fibroblast growth factor (bFGF) with IC₅₀ values of 11 and 9 nM, respectively, in an enzyme assay. It is selective for VEGFR2 and bFGF over EGFR, PDGF receptor β (PDGFRβ), and related tyrosine kinases. CP 547,632 inhibits VEGFR2 autophosphorylation induced by VEGF in porcine aortic endothelial cells transfected with VEGFR2 (IC₅₀ = 6 nM) and in a xenograft mouse model using NIH3T3/H-Ras cells (EC₅₀ = 590 nM). It decreases angiogenesis induced by VEGF or bFGF and suppresses tumor growth in athymic mice.