产品性状

PF-00562271是PF-562271的苯磺酸盐，是一种有效的，ATP竞争性，可逆的FAK抑制剂，IC50为1.5 nM，作用于Pyk2比作用于FAK效果低10倍左右，比作用于其他蛋白激酶（除了一些CDKs）选择性高100倍以上。溶解性：Soluble in DMSO (14 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), and ethanol (<1 mg/ml at 25 °C).

质量标准

PF-562271 displays selective inhibitory effects on FAK (IC50 of 1.5 nM) and Pyk2(IC50 of 14 nM) tyrosine kinase activity. In cell-based assays, PF-562271 is shown to be more selective for FAK compared to other kinase targets (IC50 of 5 nM). PF-562271 results in a dose-dependent cell proliferation inhibition in FAK WT (IC50 of 3.3 μM), FAK?/? (IC50 of 2.08 μM) and FAK kinase-deficient (KD) cells (IC50 of 2.01 μM), in 2 dimensional (2D) cultures.