FASN-IN-7

FASN-IN-7 is a potent and orally active inhibitor of human Fatty Acid Synthase (FASN). FASN-IN-7 shows enzyme inhibition on full length FASN and the FASN KR domain with IC₅₀ values of 28 and 54 nM. FASN-IN-7 effectively inhibits proliferation of multiple cancer cell types. FASN-IN-7 increases malonyl-CoA levels and decreases palmitate levels in tumor tissues^[1]. In Vitro:FASN-IN-7 (Compound 34) (4 days) strongly inhibits cell proliferation in LRS in several cancer cell lines including A2780 (ovarian), PC3M (prostate), LNCaP (prostate), OCI-LY1 (lymphoma), MV4-11 (leukemia/lymphoma/myeloma), H460 (lung), A549 (lung), and MDA-MB-468 (breast), with EC₅₀ values of 13, 25, 66, 55, 59, 36, 20 and 26 nM^[1]. In Vivo:FASN-IN-7 (3-30 mg/kg; p.o.; Twice daily; 2 days) increases malonyl-CoA levels and decreases palmitate levels in NCI-H460 lung xenograft-bearing mice^[1].