TVB-3664 is an orally available, reversible, potent, selective and highly bioavailable fatty acid synthase (FASN) inhibitor, with IC50 values of 18 nM and 12 nM for human and mouse cell palmitate synthesis, respectively. TVB-3664 significantly reduces tubulin palmitoylation and mRNA expression[2].IC50 & Target: FASN[2].In Vitro: TVB-3664 (0-1 μM, 7 days) shows anti-tumor activity in CaCo2, HT29 and LIM2405 cell lines.
TVB-3664 decreases viability in multiple tumor cell lines from solid and hematopoietic tumor types.In Vivo: TVB-3664 (3 mg/kg (Pt 2614 and Pt 2449PT) or 6 mg/kg (Pt 2402 and Pt 2449LM), oral gavage, daily, 4 weeks) treatment leads to a significant reduction in tumor volume and tumor weight in Pt 2614, Pt 2449PT, and Pt 2402 PDX models, with an average reduction in tumor weight of 30%, 37.5% and 51.5%, respectively.