MRX-2843

MRX-2843 is an orally bioavailable, small molecule inhibitor of the receptor tyrosine kinases MerTK (tyrosine-protein kinase Mer) and FLT3 (Fms-like tyrosine kinase 3). It acts by binding to and inhibiting both MerTK and FLT3, preventing their ligand-dependent phosphorylation and activation. This inhibition blocks downstream signaling pathways involved in cell proliferation and survival, leading to apoptosis and reduced proliferation in tumor cells overexpressing these kinases. MRX-2843 has demonstrated preclinical efficacy against acute myeloid leukemia (AML), including models resistant to other FLT3 inhibitors due to D835 or F691 mutations, as well as activity in MERTK-dependent AML models. The drug is being developed by Emory University/Meryx/National Cancer Institute for various hematologic malignancies such as AML, acute lymphoblastic leukemia (ALL), mixed phenotype acute leukemia, as well as solid tumors including non-small cell lung cancer.

Other names

1429882-07-4