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PI3K/Akt/mTOR-IN-2 is an inhibitor of the PI3K/Akt/mTOR pathway.1 It reduces the phosphorylation of Akt and mTOR when used at a concentration of 2 µM and decreases PI3K, Akt, and mTOR levels at 4 µM. PI3K/Akt/mTOR-IN-2 is cytotoxic to A549, BGC-823, PC3, MCF-7, and MDA-MB-231 cancer cells (IC50s = 14.81, 9.11, 9.04, 7.89, and 2.29 µM, respectively). It induces apoptosis and cell cycle arrest at the G0/G1 phase in MDA-MB-231 breast cancer cells. PI3K/Akt/mTOR-IN-2 decreases the mitochondrial membrane potential and glutathione (GSH) levels and increases reactive oxygen species (ROS) and intracellular calcium levels in MDA-MB-231 cells in a concentration-dependent manner.
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1. Design, synthesis and biological evaluation of novel 1,3,4,9-