Description
An ATR inhibitor (IC50 = 7 nM); selective for ATR over DNA-PK, ATM, and PI3Kβ (IC50s = 0.332, 1.42, and 3.27 µM, respectively); inhibits proliferation of HT-29 and LoVo colorectal cancer cells and SU-DHL-8 B lymphoma cells (IC50s = 0.16, 0.071, and 0.009 µM, respectively); reduces tumor growth in a mutant ATMK1964E-containing SU-DHL-8 and LoVo mouse xenograft models at 50 mg/kg; synergistic with carboplatin, olaparib, or radiation in various mouse xenograft models