Cayman BAY-2402234

BAY-2402234 is an inhibitor of dihydroorotate dehydrogenase (DHODH; IC₅₀ = 1.2 nM). It induces upregulation of the cell differentiation marker CD11b in MOLM-13 and HEL acute myeloid leukemia (AML) cells (EC₅₀s = 3.16 and 0.96 nM, respectively) and inhibits the proliferation of nine leukemia cell lines (IC₅₀s = 0.08-8.2 nM). BAY-2402234 induces cell cycle arrest at the g₂/M phase and apoptosis in TF-1 cells in a concentration-dependent manner. In vivo, BAY-2402234 (1.25, 2.5, and 5 mg/kg) reduces tumor volume in an MV4-11 mouse xenograft model. It also increases survival in patient-derived xenograft (PDX) mouse models of AML.

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