CP-547632 hydrochloride

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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。

CAS NO:

252003-71-7

CP-547632 hydrochloride 是一种耐受良好，口服生物可利用的 VEGFR-2 和碱性成纤维细胞生长因子 (FGF) 激酶抑制剂，IC50 分别为 11 nM 和 9 nM。CP-547632 hydrochloride 是 ATP 竞争性激酶抑制剂，相对于表皮生长因子受体，血小板衍生生长因子 β 和其他相关 TK 具有选择性。CP-547632 hydrochloride 有抗肿瘤功效。

Cas No.	252003-71-7
Canonical SMILES	O=C(NC1=C(C(N)=O)C(OCC2=C(F)C=C(Br)C=C2F)=NS1)NCCCCN3CCCC3.[H]Cl
分子式	C₂₀H₂₅BrClF₂N₅O₃S
分子量	568.86
溶解度	DMSO: 38.33 mg/mL (67.38 mM); Water:< 0.1 mg/mL (insoluble)
储存条件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	CP-547632 hydrochloride is a well-tolerated, orally-bioavailable inhibitor of the VEGFR-2 and basic fibroblast growth factor (FGF) kinases with IC50s of 11 nM and 9 nM, respectively. CP-547632 hydrochloride is an ATP-competitive kinase inhibitor and it is selective relative to epidermal growth factor receptor, platelet-derived growth factor β, and other related TKs. CP-547632 hydrochloride has antitumor efficacy[1]. CP-547632 hydrochloride (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 hydrochloride (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 hydrochloride (oral; 50 mg/kg) of a single oral dose of 50 mg/kg yieldes plasma concentrations above 500 ng/ml for 12 hours[1]. Animal Model: Mice 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.