TVB-3166 是一种口服有效的，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。它诱导细胞凋亡，抑制体内异种移植肿瘤生长。

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).

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) [1].

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 [1].

1533438-83-3

C24H24N4O

384.47

DMSO:60 mg/mL (156.06 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years