SMU-037

SMU-037 is an orally bioavailable, selective ROS1 inhibitor with potent activity (IC50= 6.8 nM) and the ability to penetrate the blood-brain barrier. It exhibits approximately 25-fold selectivity for ALK and demonstrates remarkable sensitivity to the G2032R resistance mutation. SMU-037 inhibits the phosphorylation of ROS1 and its downstream MAPK-ERK signaling pathway, leading to cell cycle arrest and apoptosis. It effectively suppresses tumor growth in both subcutaneous and intracranial xenograft mouse models. SMU-037 is applicable for research related to non-small cell lung cancer (NSCLC) .