中文名: | PF-00562271;N-甲基-N-(3-(2-((2-氧代吲哚-5-基)氨基)-5-(三氟甲基)嘧啶-4-基)氨基)甲基)吡啶-2-基)甲烷磺酰胺苯磺酸盐 |
中文别名: | PF 562271 苯磺酸盐; N-甲基-N-[3-[[[2-[(2-氧代-2,3-二氢-1H-吲哚-5-基)氨基]-5-三氟甲基嘧啶-4-基]氨基]甲基]吡啶-2-基]甲磺酰胺苯磺酸盐;PF562271 besylate; |
英文名称: | PF-00562271 |
英文别名: | PF 562271 besylate;N-[3-[[[2-[(2,3-Dihydro-2-oxo-1H-indol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]-2-pyridinyl]-N-methyl-methanesulfonamide benzenesulfonate |
CAS No.: | 939791-38-5 |
分子式: | C21H20F3N7O3S·C6H6O3S |
分子量: | 665.66 |
性状: | 属性溶解性Soluble in DMSO (14 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), and ethanol (<1 mg/ml at 25 °C).存贮条件储存温度-20°C描述产品介绍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。用途A potent inhibitor of focal adhesion kinase (FAK) and Pyk2.生化机理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. |
储存: | 储存温度-20°C |
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用途: | A potent inhibitor of focal adhesion kinase (FAK) and Pyk2. |