BAY-1895344

BAY-1895344 is an inhibitor of ataxia-telangiectasia and Rad3-related protein/kinase (ATR; IC₅₀ = 0.007 µM).^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 µM, 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 µM, respectively. It reduces tumor growth in a mutant ATM^K1964E-containing SU-DHL-8 mouse xenograft model when administered at a dose of 50 mg/kg. BAY-1895344 is synergistic with carboplatin (Item No. 13112), olaparib (Item No. 10621), or radiation in various mouse xenograft models.^1,2

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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 models. J. 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 models. Mol. Cancer Ther. 19(1), 26-38 (2020).