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

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

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

252003-71-7

C20H25BrClF2N5O3S

568.86

DMSO:38.33 mg/mL (67.38 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years