Potent, ATP-competitive inhibitor of mammalian target of rapamycin (mTOR) (IC50 = 7nm). Displays selectivity for mTOR over PI 3-Kalpha (~100-fold) and PI 3-Kgamma (~500-fold). Inhibits phosphorylation of mTORC1 and mTORC2 substrates including S6K, SGK and Akt; blocks VEGF secretion and HIF-1alpha expression. Exhibits antiproliferative effects in cancer cell lines through G1 cell cycle arrest and selective apoptosis.
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