Our studies identified PKM2-IN-1 in combination with NCT-503 as a new treatment of cancer therapy that induces cell apoptosis by the Bcl-2/caspase-3/PARP pathway and promotes G2/M phase arrest and inhibits proliferation by p53/p21/cdc2-cyclin B and mTOR/p70S6K pathways through the ROS-induced DNA damage and AMPK dependent pathways in A549 cells. This evidence concerns the gene MTOR and cancer.