Fasnall is an inhibitor of fatty acid synthase (FASN) with an IC50 value of 3.71 μM for the human recombinant enzyme.[1] It inhibits tritiated acetate incorporation into lipids (IC50 = 5.84 μM), increases ceramide accumulation, and induces the formation of lipid droplets in BT474 HER2+ breast cancer cells. Fasnall has antiproliferative activity against non-tumorigenic MCF-10A and tumorigenic MCF-7, MDA-MB-468, BT474, and SK-BR-3 breast cancer cells that directly correlates to the level of FASN expression in vitro. It reduces tumor volume and increases survival in the murine MMTV-Neu model of HER2+ breast cancer. Fasnall also potentiates carboplatin response in vivo, increasing the objective response rate of stable disease from 25% for carboplatin alone to 88% for carboplatin with fasnall.
Reference：
[1]. Alwarawrah, Y., Hughes, P., Loiselle, D., et al. Fasnall, a selective FASN inhibitor, shows potent anti-tumor activity in the MMTV-Neu model of HER2+ breast cancer. Cell Chem. Bio. 23(6), 678-688 (2016).