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CP-547632 TFA is an orally active, ATP-competitive inhibitor that potently targets VEGFR-2 and FGF kinases with IC50 values of 11 nM and 9 nM, respectively. It demonstrates selectivity for VEGFR-2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs), exhibiting antitumor efficacy [1].
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,970 | 1-2 weeks | |
50 mg | $2,580 | 1-2 weeks | |
100 mg | $3,400 | 1-2 weeks |
Description | CP-547632 TFA is an orally active, ATP-competitive inhibitor that potently targets VEGFR-2 and FGF kinases with IC50 values of 11 nM and 9 nM, respectively. It demonstrates selectivity for VEGFR-2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs), exhibiting antitumor efficacy [1]. |
Targets&IC50 | FGFR:9 nM, VEGFR2:11 nM |
In vitro | CP-547632 TFA (1-1000 nM; 1 hour) inhibits VEGF-induced VEGFR-2 phosphorylation in a dose-dependent manner, with an IC50 of 6 nM [1]. |
In vivo | CP-547632 TFA, when administered orally in doses ranging from 6.25 to 100 mg/kg/day over a period of 10-24 days, results in a dose-dependent suppression of tumor growth in Colo-205, DLD-1, and MDA-MB-231 xenografts [1]. A single oral dose of 50 mg/kg produces plasma concentrations exceeding 500 ng/ml for a duration of up to 12 hours [1]. |
Molecular Weight | 646.43 |
Formula | C22H25BrF5N5O5S |
Cas No. | 2805804-54-8 |
Storage | Shipping with blue ice. |
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