SMU-037 is an orally active and selective ROS1 inhibitor that demonstrates potent activity (IC50 = 6.8 nM) and possesses the ability to penetrate the blood-brain barrier. SMU-037 shows ~25-fold selectivity over ALK, and superior sensitivity against the G2032R mutation. SMU-037 attenuates phosphorylation of ROS1 and downstream MAPK-ERK signaling pathway, leading to cell cycle arrest and apoptosis. SMU-037 effectively suppresses tumor progression in both xenograft and intracranial mouse models. SMU-037 can be used for non-small cell lung cancer (NSCLC) research[1].
Molekulargewicht:
523.02
Formel:
C29H29ClF2N4O
Target-Kategorie:
Apoptosis,ERK,p38 MAPK,ROS Kinase
Anwendungsbeschreibung:
MCE Product type: Reference compound
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