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CP-547632 TFA
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CP-547632 TFA图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
CP-547632TFA是一种口服有效的,ATP竞争性的VEGFR-2和FGF激酶抑制剂,IC50分别为11nM和9nM。CP-547632TFA对VEGFR2和bFGF的选择性高于EGFR,PDGFRβ和相关的酪氨酸激酶(TKs)。CP-547632TFA具有抗肿瘤作用。
Canonical SMILESFC(F)(C(O)=O)F.O=C(NC1=C(C(N)=O)C(OCC2=C(F)C=C(Br)C=C2F)=NS1)NCCCCN3CCCC3
分子式C22H25BrF5N5O5S
分子量646.43
溶解度DMSO: 150 mg/mL (232.04 mM)
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.