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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)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
CP-547632 TFA 是一种口服有效的,ATP 竞争性的VEGFR-2FGF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。
生物活性

CP-547632 TFA is an orally active, ATP-competitive and potentVEGFR-2andFGFkinases inhibitor withIC50s of 11 nM and 9 nM, respectively. CP-547632 TFA is selective for VEGFR2 and bFGF overEGFR,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 IC50value of 6 nM[1].

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].

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

性状

Solid

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 mg5 mg10 mg
1 mM1.5470 mL7.7348 mL15.4696 mL
5 mM0.3094 mL1.5470 mL3.0939 mL
10 mM0.1547 mL0.7735 mL1.5470 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℃, 6 months; -20℃, 1 month (stored under nitrogen, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。