MF-438 (921605-87-0) is a potent inhibitor of stearoyl-CoA desaturase 1 (SCD1) - IC50 = 2.3 nM.1 MF-438 was potent in an in vivo mouse liver PD assay (ED50 between 1 and 3 mg/kg).1 Cancer initiating cells (CSC-like) were shown to be much more sensitive to MF-438 inhibition of SCD1 than progenitor and terminally differentiated cancer cells in a lung cancer model.2 MF-438 showed good oral bioavailability and metabolic stability making it an excellent tool for studying the effects of SCD1 in various disease models.
1) Leger et al. (2010), Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438); Bioorg. Med. Chem. Lett., 20 499
2) Noto et al. (2013), Stearoyl-CoA desaturase-1 is a key factor for lung cancer-initiating cells; Cell Death and Differ., 4 e947
3) Rodriguez-Perez et al. (2017), Altered fatty acid metabolism and reduced stearoyl-coenzyme A desaturase activity in asthma; Allergy, 72 1744 [Citation]