1429882-07-4

MRX-2843 is an inhibitor of Mer and FMS-like tyrosine kinase 3 (FLT3; IC₅₀s = 1.3 and 1 nM, respectively). It also inhibits Axl and Tyro3 (IC₅₀s = 15 and 17 nM, respectively). MRX-2843 (10-300 nM) inhibits Mer phosphorylation in MOLM-14 and MV4-11 acute myeloid leukemia (AML) cells and reduces clonal expansion of Kasumi-1 AML cells (IC₅₀ = 143.5 nM). In vivo, MRX-2843 increases survival in NOMO-1 and MOLM-14 AML mouse xenograft models when administered at doses of 65 and 50 mg/kg, respectively.

MRX-2843, is an orally available small-molecule inhibitor of both MERTK and FLT3.