TVB-3166

1533438-83-3

384.47

DMSO : 62.5 mg/mL (162.56 mM; Need ultrasonic)

Apoptosis; Metabolic Enzyme/Protease

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]. IC50 & Target: IC50: 42 nM (FASN) and 81 nM (cellular palmitate synthesis)^[1] In Vitro: TVB-3166 (0.001-10 uM; 24 hours) causes cell death in CALU-6 non-small-cell lung tumor cells with a cellular IC₅₀ value of 0.10 uM^[1].
TVB-3166 (0.02 or 0.20 uM; 7 days) inhibits palmitate synthesis and tumor cell viability in a dose-dependent manner^[1].
TVB-3166 (0.2 uM; 48 hours) inhibits beta-catenin pathway signal transduction and transcriptional activity^[1].
In Vivo: 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 uM, respectively^[1].