FT113

FT113 is an inhibitor of fatty acid synthase (FASN; IC₅₀ = 213 nM).¹ It inhibits the proliferation of PC3 human prostate cancer and MV4-11 human acute myeloid leukemia cells (IC₅₀s = 47 and 26 nM, respectively) and inhibits FASN activity in a ¹⁴C-acetate incorporation assay using BT474 human breast cancer cells (IC₅₀ = 90 nM). FT113 (25 and 50 mg/kg) reduces tumor growth and increases intratumoral levels of the FASN substrate malonyl-CoA in an MV4-11 mouse xenograft model. It also inhibits infection of HEK293T cells expressing human angiotensin-converting enzyme 2 (HEK293T-hACE2 cells) with an infectious-clone-derived mNeonGreen severe acute respiratory syndrome coronavirus 2 reporter virus (SARS-CoV-2-mNG) with an EC₅₀ value of 17 nM.²

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1. Martin, M.W., Lancia, D.R., Jr., Li, H., et al. Discovery and optimization of novel piperazines as potent inhibitors of fatty acid synthase (FASN). Bioorg. Med. Chem. Lett. 29(8), 1001-1006 (2019).

2. Chu, J., Xing, C., Du, Y., et al. Pharmacological inhibition of fatty acid synthesis blocks SARS-CoV-2 replication. Nat. Metab. 3(11), 1466-1475 (2021).