1253286-90-6

SMU-B is a highly selective, well-tolerated, and orally efficacious c-Met/ALK dual inhibitor.

SMU-B is the orally active inhibitor for ALK (IC50<0.5 nM), c-ros oncogene 1 (ROS1), c-MET (IC50=1.87 nM) and AXL (IC50=28.9 nM). SMU-B inhibits the proliferation of MKN45, H1993 and H441 with IC50s of 0.02 μM, 1.58 μM and 2.82 μM, respectively. SMU-B exhibits antitumor efficacy in mouse models[1][2].

[1] Tian Y, et al., Molecular Simulation Studies on the Binding Selectivity of Type-I Inhibitors in the Complexes with ROS1 versus ALK. J Chem Inf Model. 2017 Apr 24;57(4):977-987. DOI:10.1021/acs.jcim.7b00019
[2] Li J, et al., Aminopyridyl/Pyrazinyl Spiro[indoline-3,4'-piperidine]-2-ones As Highly Selective and Efficacious c-Met/ALK Inhibitors. ACS Med Chem Lett. 2013 Jul 12;4(8):806-10. DOI:10.1021/ml400203d