产品描述
| 溶解性 |
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| 存贮条件 | 储存温度-20°C |
| 应用 | A PI3K and FRAP inhibitor |
| 产品介绍 | Gedatolisib (PF-05212384, PKI-587)是一种高度有效的，双重PI3Kα， PI3Kγ和mTOR抑制剂，IC50分别为0.4 nM， 5.4 nM和1.6 nM。 |
| 备注 | PKI-587 is a highly potent dual inhibitor of PI3Kα, PI3Kγ and mTOR with IC50 of 0.4 nM, 5.4 nM and 1.6 nM, respectively. Phase 2. |
| 生化机理 | PKI-587 is a potent inhibitor to PI3K-α, PI3K-γ, and mTOR (FRAP) with IC50 of 0.4 nM, 5.4 nM, and 1.6 nM, respectively. PKI-587 also exhibits potency against the most frequently occurring mutant forms of PI3Kα, notably the H1047R and E545K with IC50 of 0.6 nM and 0.6 nM, respectively. PF-05212384 inhibitory actions against PI3Ks and mTORs causes tumor cell growth inhibition in MDA-361 and PC3-MM2 cell lines with IC50 of 4 nM and 13.1 nM, respectively. |
| 别名 | N-[4-[[4-(二甲基氨基)-1-哌啶基]羰基]苯基]-N'-[4-[4,6-二(4-吗啉基)-1,3,5-三嗪-2-基]苯基]脲;PKI-587;Gedatolisib; PF-05212384;PKI-587;N-[4-[[4-(Dimethylamino)-1-piperidinyl]carbonyl]phenyl]-N'-[4-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]phenyl]urea |
