BGS-2457

BGS-2457 is a small molecule inhibitor of Fms-like tyrosine kinase 3 (FLT3) developed by Bridgene Biosciences. It is the non-covalent analog of BGS-2456, specifically designed without the covalent warhead to serve as a control in mechanistic studies. In preclinical evaluations, BGS-2457 demonstrated significantly lower potency compared to BGS-2456 and its activity was not affected by the C695S mutation in FLT3, confirming that the C695 residue is the site of covalent attachment for BGS-2456. While BGS-2456 is being positioned as a potential treatment for FLT3-mutant acute myeloid leukemia (AML) due to its high selectivity over KIT, BGS-2457 primarily functions as a research tool to validate the covalent binding mode of the lead compound.