产品
编 号：F293341
分子式：C20H24BrF2N5O3S
分子量：532.4
分子式：C20H24BrF2N5O3S
分子量：532.4
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 252003-65-9
产品详情
生物活性：
CP-547632 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 is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 has antitumor efficacy.
体内研究：
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. CP-547632 (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 (1-1000 nM; 1 hours) inhibits VEGF-stimulated VEGFR-2 phosphorylation in a dose-dependent fashion, with an IC50 value of 6 nM.
CP-547632 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 is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 has antitumor efficacy.
体内研究：
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. CP-547632 (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 (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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