CP-547632 TFA

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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。

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-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。

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 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℃, 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。