CP-547632 TFA |
| Catalog No.GC60726 |
CP-547632 TFA는 각각 11nM 및 9nM의 IC50을 갖는 경구 활성, ATP-경쟁적 및 강력한 VEGFR-2 및 FGF 키나제 억제제입니다. CP-547632 TFA는 EGFR, PDGFRβ 및 관련 티로신 키나제(TK)보다 VEGFR2 및 bFGF에 대해 선택적입니다. CP-547632 TFA는 항종양 효능이 있습니다.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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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].
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[1]. Western Blot Analysis[1] Cell Line: Serum-deprived cells
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]
[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.
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