CG-3-246

CG-3-246 is an experimental, polypharmacologic hybrid single-molecule inhibitor designed to simultaneously target B-cell lymphoma 2 (BCL-2) and Fms-like tyrosine kinase 3 (FLT3). It was developed by researchers at the University of Florida by chemically tethering the BCL-2 inhibitor venetoclax to the FLT3 inhibitor gilteritinib via their solvent-exposed domains. The compound is intended for the treatment of acute myeloid leukemia (AML), a disease often characterized by the co-expression or mutational activation of these two pathways. While CG-3-246 demonstrates dual inhibitory activity, preclinical studies published in 2024 indicated that the physical combination (polypharmacy) of venetoclax and gilteritinib provided superior antileukemic activity compared to the hybrid molecule.

Other names

VEN-GIL hybrid inhibitorBCL-2/FLT3 hybrid inhibitor