1794791-66-4
1794791-66-4 結構式
基本信息
英文別名
WYE 354-d34-[6-[4-[[(Methoxy-d3)carbonyl]aMino]phenyl]-4-(4-Morpholinyl)-1H-pyrazolo[3,4-d]pyriMidin-1-yl]-1-piperidinecarboxylic Acid Methyl Ester
應用領域
用途1
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.