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.
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产品名称 | FAK ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Defactinib | ✔ | 99%+ | |||||||||||||||||
NVP-TAE 226 |
++
FAK, IC50: 5.5 nM PYK2, IC50: 3.5 nM |
IGF-1R,Insulin Receptor | 98+% | ||||||||||||||||
PF-573228 |
+
FAK, IC50: 4 nM |
98% | |||||||||||||||||
Solanesol | ✔ | 90% +(HPLC) | |||||||||||||||||
PF-431396 |
++
FAK, IC50: 2 nM PYK2, IC50: 11 nM |
99%+ | |||||||||||||||||
PND-1186 |
++++
FAK, IC50: 1.5 nM |
99%+ | |||||||||||||||||
PF-562271 |
++++
FAK, IC50: 1.5 nM PYK2, IC50: 13 nM |
99%+ | |||||||||||||||||
GSK2256098 |
++++
FAK, Ki: 0.4 nM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
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] |
Dose | Rat: 10 mg/kg, 30 mg/kg[3] (p.o.) Mice: 5 mg/g[4] (i.v.) |
Administration | p.o., i.v. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.97mL 0.39mL 0.20mL |
9.87mL 1.97mL 0.99mL |
19.74mL 3.95mL 1.97mL |
CAS号 | 717906-29-1 |
分子式 | C22H21F3N6O3S |
分子量 | 506.501 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,Room temperature |
溶解度 | |
动物实验配方 |