BAY-1895344 is an inhibitor of ataxia-telangiectasia and Rad3-related protein/kinase (ATR; IC50 = 0.007 ?M).1,2 It is selective for ATR over DNA protein kinase (DNA-PK), ataxia-telangiectasia mutated kinase (ATM), and PI3Kβ (IC50s = 0.332, 1.42, and 3.27 ?M, respectively).1 BAY-1895344 inhibits proliferation of HT-29 and LoVo colorectal cancer cells and SU-DHL-8 B lymphoma cells with IC50 values of 0.16, 0.071, and 0.009 ?M, respectively. It reduces tumor growth in a mutant ATMK1964E-containing SU-DHL-8 mouse xenograft model when administered at a dose of 50 mg/kg. BAY-1895344 is synergistic with carboplatin , olaparib , or radiation in various mouse xenograft models.1,2
1.Lücking, U., Wortmann, L., Wengner , A.M., et al.Damage incorporated: Discovery of the potent, highly selective, orally available ATR inhibitor BAY 1895344 with favorable pharmacokinetic properties and promising efficacy in monotherapy and in combination treatments in preclinical tumor modelsJ. Med. Chem.63(13)7293-7325(2020) 2.Wengner, A.M., Siemeister, G., Lücking, U., et al.The novel ATR inhibitor BAY 1895344 Is efficacious as monotherapy and combined with DNA damage-inducing or repair-compromising therapies in preclinical cancer modelsMol. Cancer Ther.19(1)26-38(2020)