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Beschreibung

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 µ,M ATP) with much reduced activity against PI 3-Kalpha or PI 3-Kgamma (IC50 = 1.89 and 7.37 µ,M, respectively) and little or no activity toward 24 other kinases (IC50 >50 µ,M). 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 µ,M) 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.