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编 号:F756088
分子式:C22H25BrF5N5O5S
分子量:646.43
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生物活性:
CP-547632 TFA is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s 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 TFA has antitumor efficacy.

体内研究:
CP-547632 TFA (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. CP-547632 TFA (oral; 50 mg/kg; a single oral dose) yieldes plasma concentrations above 500 ng/ml for 12 hours. Animal Model:Athymic female mice (CD-1 nu/nu) bearing tumors (75-150 mm in size)
Dosage:6.25, 12.5, 25, 50, 100 mg/kg
Administration:PO; daily; 10-24 days
Result:Caused a dose-dependent inhibition of growth in Colo-205, DLD-1, and MDA-MB-231 xenografts.
Animal Model:Female athymic mice bearing H-Ras tumor
Dosage:50 mg/kg
Administration:Oral
Result:A single oral dose of 50 mg/kg yielded plasma concentrations above 500 ng/ml for 12 hours.

体外研究:
CP-547632 TFA (1-1000 nM; 1 hours) inhibits VEGF-stimulated VEGFR-2 phosphorylation in a dose-dependent fashion, with an IC50 value of 6 nM.
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