产品描述
| 沸点 | ~594.2 °C at 760 mmHg |
| 折光率 | ~1.69 |
| 溶解性 | DMSO ≥96mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL |
| 存贮条件 | 储存温度-20°C |
| 密度 | 1.5000 |
| 应用 | A potent, specific, and ATP-competitive inhibitor to mTOR with IC50 of 5 nM |
| 产品介绍 | WYE-354是ATP竞争性mTOR抑制剂，IC50为5 nM，能阻断mTORC1/P-S6K(T389)和mTORC2/P-AKT(S473)，比对PI3Kα和PI3Kγ的抑制性强100倍和500倍。 |
| 生化机理 | WYE-354 is an inhibitor of several PI3Ks at micromolar levels. WYE-354 is an effective inhibitor of both mTORC1 and mTORC2 in HEK293 cells. WYE-354 significantly blocks mTOR signaling and Akt activation in U87MG and MDA361 cells. WYE-354 is a potent inhibitor of proliferation in tumor cell lines including MDA-MB-361, MDA-MB-231, MDA-MB-468, LNCap, A498, and HCT116. WYE-354 induces apoptosis which is accompanied by G1 cell cycle arrest and caspases activation. WYE-354 inhibits both mTORC1 and mTORC2 signaling, as revealed by dephosphorylation of S6 ribosomal protein and Akt, respectively, in endothelial HUVEC cells. WYE-354 activates mitogen-activated protein kinase (MAPK) signaling, which may be due to its inhibition of mTORC1. |
| 别名 | WYE 354; WYE354；4-[6-[4-[(甲氧羰基)氨基]苯基]-4-(4-吗啉基)-1H-吡唑并[3,4-d]嘧啶-1-基]-1-哌啶羧酸甲酯;WYE 354;WYE354； 4-[6-[4-[(Methoxycarbonyl)amino]phenyl]-4-(4-morpholinyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinecarboxylic acid methyl ester |
