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MRX-2843 is an inhibitor of Mer and FMS-like tyrosine kinase 3 (FLT3; IC50s = 1.3 and 1 nM, respectively).1 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).2 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.
WARNING This product is not for human or veterinary use.
1. UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor. J. Med. Chem. 57(16), 7031-7041 (2014).
2. The MERTK/FLT3 inhibitor MRX-