mTOR Kinase Inhibitor II, WYE-354 – CAS 1062169-56-5 – Calbiochem

Descrição detalhada : A cell-permeable pyrazolopyrimidine compound that acts as a potent and ATP-competitive mTOR inhibitor (IC50 = 5 nM with S6K as the substrate and 100 µM ATP) with much reduced activity against PI 3-Kalpha or PI 3-Kgamma (IC50 = 1.89 and 7.37 µM, respectively) and little or no activity toward 24 other kinases (IC50 >50 µM). 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 on 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.
Sinónimos : mTOR Kinase Inhibitor II, WYE-354 - CAS 1062169-56-5 - Calbiochem; Methyl-4-(6-{4-[(methoxycarbonyl)amino]phenyl}-4-morpholin-4-yl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate, mTOR Inhibitor II
Fórmula molecula r: C24H29N7O5
Armazenamento : -20C
Embalagem : 1X5MG