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 |
应用 | A potent inhibitor of focal adhesion kinase (FAK) and Pyk2. |
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。 |
备注 | PF-00562271 is the benzenesulfonate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, excep |
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. |
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; 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 |
PF 562271 苯磺酸盐
PF-00562271 (订货以英文为准)
编号:P129811
CAS号:939791-38-5
分子式:C27H26F3N7O6S2
分子量:665.66
产品名称 | PF-00562271 |
中文名称 | PF 562271 苯磺酸盐 |
CAS号 | 939791-38-5 |
分子式(M.F.) | C27H26F3N7O6S2 |
分子量(M.W.) | 665.66 |
储存条件 | -20°C储存 |
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