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]
