CP-547632 TFA is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC 50 s of 11 nM and 9 nM, respectively. CP-547632 TFA is selective for VEGFR2 and bFGF over EGFR , PDGFRβ , and related tyrosine kinases (TKs). CP-547632
In Vitro:CP-547632 TFA (1-1000 nM; 1 hours) inhibits VEGF-stimulated VEGFR-2 phosphorylation in a dose-dependent fashion, with an IC 50 value of 6 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot
In Vivo:CP-547632 TFA (p.o.; 6.25-100mg/kg/day; for 10-24 days) causes a dose-dependent inhibition of growth in Colo-205, DLD-1, and MDA-MB-231 xenografts. CP-547632 TFA (oral; 50mg/kg; a single oral dose) yieldes plasma concentrations above 500 ng/ml for
Biological Activity:CP-547632 TFA is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC 50 s of 11 nM and 9 nM, respectively. CP-547632 TFA is selective for VEGFR2 and bFGF over EGFR , PDGFRβ , and related tyrosine kinases (TKs). CP-547632