PF15 TFA is a PROTAC connected by ligands for FLT3 kinase and CRBN. PF15 TFA is a high selective FLT3-ITD degrader,with a DC50 of 76.7 nM. PF15 TFA significantly inhibits the proliferation of FLT3-ITD-positive cells,can down-regulate the phosphorylation of FLT3 and STAT5. PF15 TFA also inhibits tumor growth in mouse models and can be used in study of leukemia.
References:
[1]. Chen Y, et al. Degrading FLT3-ITD protein by proteolysis targeting chimera (PROTAC). Bioorg Chem. 2022 Feb;119:105508.
















