SMU-037

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].

Product Specifications

UNSPSC

12352005

Target

Apoptosis; ERK; p38 MAPK; ROS Kinase

Related Pathways

Apoptosis; MAPK/ERK Pathway; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Smiles

C[C@H](C1=CC(F)=CC=C1C2=CC=C(C=C2)F)OC3=C(N=CC(C4=CC=C(C=C4)N5CCNCC5)=C3)N.Cl

Molecular Formula

C29H29ClF2N4O

Molecular Weight

523.02

References & Citations

[1]Liu S, et al. Discovery of novel 3-Benzyloxyaminopyridines as orally available and intracranially active selective ROS1 inhibitors for combating the resistant ROS1G2032R mutation. Eur J Med Chem. 2025 Dec 15;300:118089.