CP-547632 hydrochloride
目录号: PL03334 纯度: ≥99%
CAS No. :252003-71-7
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中文名称
CP-547632 hydrochloride
英文名称
CP-547632 hydrochloride
英文别名
OKR4BWW90F;4-Isothiazolecarboxamide, 3-((4-bromo-2,6-difluorophenyl)methoxy)-5-((((4-(1-pyrrolidinyl)butyl)amino)carbonyl)amino)-, hydrochloride (1:1);3-((4-Bromo-2,6-difluorobenzyl)oxy)-5-(3-(4-(pyrrolidin-1-yl)butyl)ureido)isothiazole-4-carboxylic acid amide hydrochloride (1:1);3-((4-Bromo-2,6-difluorobenzyl)oxy)-5-(3-(4-(pyrrolidin-1-yl)buty;Unii-okr4bww90F;CP-547632 hydrochloride
Cas No.
252003-71-7
分子式
C20H25BrClF2N5O3S
分子量
568.86
包装储存
4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
产品详情
CP-547632 hydrochloride 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 11 nM 和 9 nM。CP-547632 hydrochloride 对 VEGFR2 和 bFGF 的选择性高于 EGFR,PDGFRβ 和相关的酪氨酸激酶 (TKs)。CP-547632 hydrochloride 具有抗肿瘤作用。
生物活性
CP-547632 hydrochloride is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC 50 s of 11 nM and 9 nM, respectively. CP-547632 hydrochloride is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 hydrochloride has antitumor efficacy.
性状
Solid
IC50 & Target[1][2]
VEGFR-2 11 nM (IC50) FGFR 9 nM (IC50
体外研究(In Vitro)
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. has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analysis
体内研究(In Vivo)
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.
CP-547632 hydrochloride (oral; 50 mg/kg; a single oral dose) yieldes plasma concentrations above 500 ng/ml for 12 hours.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
ClinicalTrial
参考文献
[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.
溶解度数据
In Vitro: DMSO : 33.33 mg/mL (58.59 mM; ultrasonic and warming and heat to 60°C)H2O : 1 mg/mL (1.76 mM; ultrasonic and adjust pH to 12 with NaOH)
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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