BAY-204

BAY-204 is a potent, selective, and orally bioavailable small molecule inhibitor of Casein Kinase 1 Alpha 1 (CSNK1A1), developed through a collaboration between Bayer and the Broad Institute. It utilizes a tetrahydro-pyrrolopyridinone scaffold and acts as an ATP-competitive inhibitor. CSNK1A1 is a serine/threonine kinase involved in critical cellular processes, including cell division, beta-catenin signaling, and TP53 activation. Preclinical studies have demonstrated anti-tumor efficacy in solid tumor models, particularly those with high expression of FAM83 family members (FAM83B and FAM83H), which mediate the subcellular localization of CSNK1A1. Efficacy has been observed in murine xenograft models of colorectal cancer, gastric cancer, urothelial cancer, and diffuse large B-cell lymphoma (DLBCL).