KAN0438757 (KAN-0438757) is a potent, selective PFKFB3 inhibitor, the ester prodrug of KAN0438241 with enhanced cell permeability.
KAN0438757 impairs recruitment of ribonucleotide reductase M2 and deoxynucleotide incorporation upon DNA repair, and reduces dNTP levels.
KAN0438757 selectively inhibits proliferation of transformed cells while sparing nontransformed cells.
KAN0438757 demonstrates significant suppression of intracellular F-2,6-P2 levels with sub µM IC50 values in cell lines representing pancreatic, gastric, and colon cancer (IC50=0.24 uM in Mia Paca-2 cells).
