TVB-3166 是一种口服有效，可逆和选择性脂肪酸合成酶 (FASN) 抑制剂，对于 FASN 和细胞棕榈酸酯合成的 IC50 分别为 42 nM 和 81 nM。TVB-3166 诱导细胞凋亡，并抑制体内异种移植肿瘤的生长。
货号:ajcx15206
CAS:1533438-83-3
分子式:C24H24N4O
分子量：384.47
溶解度:DMSO: 62.5 mg/mL (162.56 mM)
纯度：98%
存储：Store at -20°C
库存： 现货

Background:

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.