HG106 (HG 106) is a potent, selective SLC7A11 inhibitor, selectively kills KRAS-mutant lung adenocarcinoma (LUAD) cells.
HG106 exerts substantial cytotoxic effects on KRAS-mutant H441 cells, which are strikingly reduced by addition of β-mercaptoethanol and l-cysteine.
HG106 preferentially decreases the viability of KRAS-mutant LUAD cells (A549 cells IC50=3.7 uM), dose-dependently reduces the oxygen consumption rate and disrupted MMP in A549 and H441 cells.
HG106 significantly induced apoptosis in KRAS-mutant LUAD cells and inhibited colony formation.
HG106 exhibits potent in vivo efficacy in a patient-derived xenograft (PDX) model of LUAD harboring a G12V mutation in KRAS.
