GPX4-IN-6

A covalent GPX4 inhibitor (IC50 = 130 nM), inhibits the growth of MDA-MB-468, BT-549, and MDA-MB-231 cells (IC50s = 12, 3.4, and 8 nM, respectively), increases lipid peroxidation and MDA levels in MDA-MB-231 cells at 10 and 20 µM, decreases mitochondrial volume and induces degradation of mitochondrial crests and outer membranes in MDA-MB-231 cells at 20 µM, reduces tumor volume and weight, without affecting body weight, in an MDA-MB-231 mouse xenograft model at 10 or 20 mg/kg per day. Formulation: A solid. InChI: InChI=1S/C18H17BrFNO5/c1-23-15-8-12(9-16(24-2)18(15)20)21(17(22)10-19)11-3-4-13-14(7-11)26-6-5-25-13/h3-4,7-9H,5-6,10H2,1-2H3. InChIKey: RKMUVAANQXYLLV-UHFFFAOYSA-N. SMILES: O=C(CBr)N(C1=CC(OC)=C(C(OC)=C1)F)C2=CC=C3OCCOC3=C2