TVB-3664 是一种具有口服具有活力的、选择性的、可逆的、具有高生物利用度的脂肪酸合酶抑制剂，其对人和老鼠棕榈酸酯合成的IC50分别为 18 nM 和 12 nM。可显著抑制微管蛋白棕榈酰化和 mRNA表达。

TVB-3664 significantly decreases tubulin palmitoylation and mRNA expression. TVB-3664 is a reversible and highly bioavailable fatty acid synthase inhibitor (IC50: 18 nM and 12 nM for human and mouse cell palmitate synthesis, respectively).

TVB-3664 reduces viability in multiple tumor cell lines from solid and hematopoietic tumor types. TVB-3664 (0-1 μM, 7 days) displays anti-tumor activity in CaCo2, HT29, and LIM2405 cell lines [1].

In Pt 2614, Pt 2449PT, and Pt 2402 PDX models, TVB-3664 (3 mg/kg or 6 mg/kg, oral gavage, daily, 4 weeks) treatment leads to a significant reduction in tumor volume and tumor weight, with an average reduction in tumor weight of 30%, 37.5%, and 51.5%, respectively [1].

2097262-58-1

C25H23F3N4O2

468.47

DMSO:8 mg/mL (17.08mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years