A FASN inhibitor
TVB-3166 is an inhibitor of fatty acid synthase (FASN; IC50 = 0.042 ?M).1 It inhibits the biosynthesis of palmitate in Calu-6 non-small cell lung cancer (NSCLC) cells and MRC-5 lung fibroblasts in a concentration-dependent manner. TVB-3166 (0.2 ?M) induces apoptosis in Calu-6, as well as 22Rv1 prostate cancer, cells. It reduces tumor growth in an OVCAR-8 mouse xenograft model and K-Ras-wild-type or -mutant patient-derived xenograft (PDX) mouse models when administered at a dose of 60 mg/kg. TVB-3166 (50 mg/kg) also reduces lung viral titers in mice infected with respiratory syncytial virus A (RSV-A).2
1.Ventura, R., Mordec, K., Waszczuk, J., 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 expressionEBioMedicine2(8)808-824(2015) 2.Ohol, Y.M., Wang, Z., Kemble, G., et al.Direct inhibition of cellular fatty acid synthase impairs replication of respiratory syncytial virus and other respiratory virusesPLoS One10(12)e0144648(2015)
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