CP-547632 TFA

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CP-547632 TFA  纯度: 98.04%

CP-547632 TFA 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 TFA 对 VEGFR2 和 bFGF 的选择性高于 EGFR，PDGFRβ 和相关的酪氨酸激酶 (TKs)。CP-547632 TFA 具有抗肿瘤作用。

CP-547632 TFA

CP-547632 TFA Chemical Structure

规格 价格 是否有货
10 mM * 1 mL in DMSO ￥1350 询问价格 & 货期
5 mg ￥950 询问价格 & 货期
10 mg ￥1700 询问价格 & 货期
25 mg ￥3500 询问价格 & 货期
50 mg ￥5800 询问价格 & 货期
100 mg ￥9500 询问价格 & 货期

* Please select Quantity before adding items.

CP-547632 TFA 的其他形式现货产品:

CP-547632 CP-547632 hydrochloride

生物活性

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].

IC50 & Target[1]

VEGFR2

11 nM (IC50)

FGFR

9 nM (IC50)

体外研究
(In Vitro)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: Serum-deprived cells
Concentration: 1, 4, 16, 63, 250, 1000 nM
Incubation Time: 1 hours
Result: Inhibited VEGF-stimulated VEGFR-2 phosphorylation in a dose-dependent fashion.

体内研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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.

Clinical Trial

分子量

646.43

Formula

C22H25BrF5N5O5S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, stored under nitrogen, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
溶解性数据
In Vitro: 

DMSO : 150 mg/mL (232.04 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5470 mL 7.7348 mL 15.4696 mL
5 mM 0.3094 mL 1.5470 mL 3.0939 mL
10 mM 0.1547 mL 0.7735 mL 1.5470 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
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.

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