TVB-3166

TVB-3166 induces apoptosis and inhibits in-vivo xenograft tumor growth. TVB-3166 is a reversible and selective fatty acid synthase inhibitor (IC50s: 42 nM and 81 nM for biochemical FASN and cellular palmitate synthesis, respectively) . (In Vitro) :TVB-3166 (0.2 μM; 48 hours) inhibits β-catenin pathway signal transduction and transcriptional activity. TVB-3166 (0.02 or 0.20 μM; 7 days) suppresses palmitate synthesis and tumor cell viability in a dose-dependent manner. TVB-3166 (0.001-10 μM; 24 hours) induces cell death in CALU-6 non-small-cell lung tumor cells (cellular IC50: 0.10 μM) . (In Vivo) :TVB-3166 (Oral gavage; 30-100 mg/kg/day) has the concentration is approximately 3-fold higher in plasma than the tumor. TVB-3166 (Oral gavage; 30-100 mg/kg/day) inhibits xenograft tumor growth. The 100 and 30 mg/kg groups had plasma and tumor concentrations of 7 and 2.9 μM, respectively .