CP-547632 is a well-tolerated, orally-bioavailable inhibitor of the VEGFR-2 and basic fibroblast growth factor (FGF) kinases (IC50s: 11 nM and 9 nM) with antitumor efficacy.

CP-547632 (1-1000 nM; 1 hours) inhibits VEGF-stimulated VEGFR-2 phosphorylation with a dose-dependent fashion (IC50: 6 nM).

CP-547632 (p.o.; 50 mg/kg) yieldes plasma concentrations above 500 ng/ml for 12 hours. CP-547632 (p.o.; 6.25-100 mg/kg/day; for 10-24 days) causes a dose-dependent inhibition of growth in Colo-205, DLD-1, and MDA-MB-231 xenografts.

252003-65-9

C20H24BrF2N5O3S

532.4

DMSO:115 mg/mL (216.00 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years