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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[1]. | [in vivo]
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[1].
CP-547632 TFA (oral; 50 mg/kg; a single oral dose) yieldes plasma concentrations above 500 ng/ml for 12 hours[1].
| Animal Model: | Athymic female mice (CD-1 nu/nu) bearing tumors (75-150 mm in size)[1] | | 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.
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| Animal Model: | Female athymic mice bearing H-Ras tumor[1] | | 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.
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| [IC 50]
VEGFR2: 11 nM (IC50); FGFR: 9 nM (IC50) | [References]
[1] Beebe JS, et al. Pharmacological characterization of CP-547,632, a novel vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for cancer therapy. Cancer Res. 2003 Nov 1;63(21):7301-9. PMID:14612527 |
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