PFK-158

PFK-158 is a small molecule inhibitor targeting the enzyme 6-phosphofructo-2-kinase/fructose 2,6-bisphosphatase isoform 3 (PFKFB3), which plays a key role in regulating glycolysis by synthesizing fructose 2,6-bisphosphate (F2,6BP), an activator of phosphofructokinase 1 (PFK1). By inhibiting PFKFB3, PFK-158 reduces glycolytic flux and glucose uptake in cancer cells, leading to decreased cell proliferation and tumor growth. It has demonstrated broad anti-tumor activity in preclinical models of various cancers including breast, lung, glioblastoma, ovarian, pancreatic, melanoma and colon cancers. The drug was developed originally at the University of Louisville and is being developed by Advanced Cancer Therapeutics primarily for treatment of solid tumors. It has undergone Phase I clinical trials evaluating safety and dose escalation. PFK‑158 also shows potential synergy with other chemotherapeutic agents such as carboplatin and paclitaxel especially in chemoresistant cancer models[1][2][5][9][10].

Other names

2-Propen-1-one, 1-(4-pyridinyl)-3-(7-(trifluoromethyl)-2-quinolinyl)(E)-1-(pyridin-4-yl)-3-[7-(trifluoromethyl)quinolin-2-yl]prop-2-en-1-onePFK-158 free basePFK158 free basePFK 158 free base