TVB-3166

TVB-3166 is an orally-available, reversible, and selective fatty acid synthase (FASN) inhibitor with IC50s of 42 nM and 81 nM for biochemical FASN and cellular palmitate synthesis, respectively. TVB-3166 induces apoptosis, and inhibits in-vivo xenograft tumor growth[1].

TVB-3166 (0.001-10 μM; 24 hours) causes cell death in CALU-6 non-small-cell lung tumor cells with a cellular IC50 value of 0.10 μM[1]. TVB-3166 (0.02 or 0.20 μM; 7 days) inhibits palmitate synthesis and tumor cell viability in a dose-dependent manner[1]. TVB-3166 (0.2 μM; 48 hours) inhibits β-catenin pathway signal transduction and transcriptional activity[1]. Cell Proliferation Assay[1] Cell Line: CALU-6 tumor cells

TVB-3166 (Oral gavage; 30-100 mg/kg/day) inhibits xenograft tumor growth[1]. TVB-3166 (Oral gavage; 30-100 mg/kg/day) has the concentration is approximately 3-fold higher in plasma than tumor. The 100 and 30 mg/kg groups had plasma and tumor concentrations of 7 and 2.9 μM, respectively[1]. Animal Model: Female BALB-c-nude mice[1]

[1]. Ventura R, et al. Inhibition of de novo Palmitate Synthesis by Fatty Acid Synthase Induces Apoptosis in Tumor Cells by Remodeling Cell Membranes, Inhibiting Signaling Pathways, and Reprogramming Gene Expression. EBioMedicine. 2015 Jul 2;2(8):808-24.