TVB-3166 is an orally-available, reversible, potent, and selective fatty acid synthase (FASN) inhibitor with biochemical IC50 of 42 nM.
TVB-3166 inhibits cellular palmitate synthesis with IC50 of 60 nM, inhibits the keto-reductase enzymatic function of FASN.
TVB-3166 specifically disrupts lipid raft architecture, inhibits biological pathways such as lipid biosynthesis, PI3K-AKT-mTOR and β-catenin signal transduction, and inhibits expression of oncogenic effectors such as c-Myc in cancer cells.
TVB-3166 demonstrates anti-tumor activities in biologically diverse preclinical tumor models.
