Biological Activity
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].
In Vitro
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 Concentration: 0.001, 0.01, 0.1, 1, 10 μM Incubation Time: 24 hours Result: Caused cell death in CALU-6 non-small-cell lung tumor cells with a cellular IC50 value of 0.10 μM. Cell Viability Assay[1] Cell Line: 90 different tumor cell lines (such as CALU-6 NSCLC cell line, NCI-H1975 NSCLC cell line) Concentration: 0.02 or 0.20 μM Incubation Time: 7 days Result: Dose-dependent induction of cell death was observed in all tumor cell lines. Western Blot Analysis[1] Cell Line: COLO-205 and A549 cells Concentration: 0.2 μM Incubation Time: 48 hours Result: Inhibited β-catenin pathway signal transduction and transcriptional activity.
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 μM, respectively[1]. Animal Model: Female BALB-c-nude mice[1] Dosage: 30, 60, or 100 mg/kg Administration: Oral gavage; once daily Result: Inhibited xenograft tumor growth. Animal Model: Female BALB-c-nude mice[1] Dosage: 30, 60, or 100 mg/kg (Pharmacokinetic Study) Administration: Oral gavage; once daily Result: The concentration was 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.
References & source
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.