BGS-2456

BGS-2456 is a novel, potent, and highly selective covalent inhibitor of Fms-like tyrosine kinase 3 (FLT3), currently in preclinical development for the treatment of FLT3-mutant acute myeloid leukemia (AML). Developed by Bridgene Biosciences, BGS-2456 distinguishes itself from other FLT3 tyrosine kinase inhibitors (TKIs) by its exceptional selectivity against KIT, a related kinase whose inhibition often leads to dose-limiting myelosuppression. The compound forms an irreversible covalent bond with the C695 residue of FLT3. Preclinical studies demonstrate that BGS-2456 maintains potent activity against common resistance-conferring mutations, including FLT3-ITD, D835Y, and the gatekeeper F691L mutation, while sparing normal hematopoietic progenitor cells in vitro.