Description | A dual inhibitor of mTOR and DNA-PK (IC50s = 0.021 and 0.013 µM, respectively); selective for mTOR and DNA-PK over PI3Kα, ATM, and ATR (IC50s = 0.85, >30, and >30 µM, respectively); inhibits growth in a panel of 123 cancer cell lines, including breast, head and neck, and lung cancer cells (GI50s = 0.015-1.77 µM); inhibits NHEJ in CAL-51, MDA-MB-231, PC3, and HCT116 cells (IC50s = 3.15, 2.16, 2.72, and 6.35 µM, respectively); reduces tumor growth in a PC3 prostate cancer mouse xenograft model at 0.25, 0.5, and 1 mg/kg twice per day |