化学性质:
规格 | 25mg |
CAS | 1197160-78-3 |
别名 |
|
化学名 | 1-[4-[4-(dimethylamino)piperidine-1-carbonyl]phenyl]-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea |
分子式 | C32H41N9O4 |
分子量 | 615.73 |
溶解度 | ≥ 15.4mg/mL in DMSO with gentle warming |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
PF-05212384 is an inhibitor of PI3K/mTOR with IC50 values of 0.4nM, 6nM, 8nM, 6nM and 1.4nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and mTOR, respectively [1].
PF-05212384 is a pan-PI3K/mTORinhibitor and shows to be highly selective for PI3K and mTOR. Besides the wt P13K, PF-05212384 can also inhibit mutant P13K with IC50 values of 0.6nM for both H1047R and E545K mutants. In cellular assay, PF-05212384 potently inhibits tumor growth in MDA-361 and PC3-MM2 cell lines with IC50 values of 4nM and 13.1nM, respectively. Meanwhile, PF-05212384 suppresses the phosphorylation of PI3K/mTOR signaling pathway proteins in cells. It inhibits the phosphorylation of Akt as well as the Akt effector proteins including GSK3 kinase, ENOS and PRAS 40. Moreover, PF-05212384 has potent anti-tumor activity in a variety of xenograft models including H1975, BT474, HCT116, H1975 and U87MG [1, 2]
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