|N-甲基-N-(2-(((2-((2-氧代二氢吲哚-5-基)氨基)-5-(三氟甲基)嘧啶-4-基)氨基)甲基)苯基)甲磺酰胺|CsnPharm

CAS No.: 717906-29-1

N-Methyl-N-(2-(((2-((2-oxoindolin-5-yl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)methyl)phenyl)methanesulfonamide Catalog No. CSN13426

Synonyms: PF-431396

PF-431396 is dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor (IC50 values are 2 and 11 nM respectively), PF-431396 has a Kd value of 445 nM for BRD4.

规格	价格	促销价格	库存	数量

400-920-2911

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400-920-2911

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Pyk2

IC50:11nM FAK

IC50:2nM Bromodomain 4

Kd:445nM
描述PYK2 (proline-rich tyrosine kinase 2) and Pyk2 (proline-rich tyrosine kinase 2) are non-receptor protein tyrosine kinases that are involved in cell proliferation, migration and survival. PF-431396 is a dual inhibitor of both PYK2 and FAK with IC50 values of 11nM and 2nM, respectively. Treatment with PF-431396 ranging in 0.1-1μM on hMSC led to a modest albeit significant increase in day 7 alkaline phosphatase activity^[1]. Suppression of Pyk2 and FAK by PF-431396 at concentration of 2.5μM to A20 cells can inhibit B cell spreading induced by BCR/integrin co-stimulation or integrin engagement^[2].
作用机制PF-431396 is an ATP-competitive inhibitor of FAK kinases which can occupy the nucleotide binding pocket, with the pyrimidine ring located in the adenine pocket.^[1]
动物研究
剂量
Rat: 10 mg/kg, 30 mg/kg^[3] (p.o.) Mice: 5 mg/g^[4] (i.v.)

给药途径
p.o., i.v.

动物研究
剂量	Rat: 10 mg/kg, 30 mg/kg^[3] (p.o.) Mice: 5 mg/g^[4] (i.v.)
给药途径	p.o., i.v.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9743 mL
- 9.8717 mL
- 19.7433 mL
- 5 mM
- 0.3949 mL
- 1.9743 mL
- 3.9487 mL
- 10 mM
- 0.1974 mL
- 0.9872 mL
- 1.9743 mL

技术信息

CAS号

717906-29-1

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H21F3N6O3S

运输

蓝冰

分子量

506.50

别名

PF-431396

溶解度

DMSO	99.0 mg/mL (195.5 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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靶点	Description	IC50
Pyk2		IC50:11nM
FAK		IC50:2nM
Bromodomain 4		Kd:445nM

N-Methyl-N-(2-(((2-((2-oxoindolin-5-yl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)methyl)phenyl)methanesulfonamide Catalog No. CSN13426

靶点选择性

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