WYE 354-d3 基本信息
中文名称 | WYE 354-d3 |
---|---|
中文同义词 | |
英文名称 | WYE 354-d3 |
英文同义词 | WYE 354-d3;4-[6-[4-[[(Methoxy-d3)carbonyl]aMino]phenyl]-4-(4-Morpholinyl)-1H-pyrazolo[3,4-d]pyriMidin-1-yl]-1-piperidinecarboxylic Acid Methyl Ester |
CAS号 | 1794791-66-4 |
分子式 | C24H29N7O5 |
分子量 | 495.54 |
EINECS号 | |
相关类别 | Amines;Aromatics;Heterocycles;Intermediates & Fine Chemicals;Isotope Labelled Compounds;Pharmaceuticals;Protein Kinase Inhibitors and Activators |
Mol文件 | 1794791-66-4.mol |
结构式 | ![]() |
WYE 354-d3 性质
A labelled pyrazolopyrimidines derivative that is a potent and ATP-competitive mTOR inhibitor with much reduced activity against PI 3-Kα or PI 3-Kγ. WYE-354 is equally potent against mTORC1 and mTORC2 activities in HEK293 immune complex kinase assays using S6K and Akt as the respective substrate (IC50 <200 nM; [ATP] = 100 μM) and effectively blocks cellular phosphorylation of S6K on T389 and Akt o n S473 both in cultures and in a murine xenograft model, resulting in a significant suppression of PC3MM2-derived tumor growth (by 86% on day 7; 50 mg/kg, i.p twice per day) in vivo.