BOS172722

Description: BOS172722 is a novel, potent and selective inhibitor of monopolar spindle 1 (MPS1) with IC50 of 2-11 nM. BOS172722 showed high bioavailability in all threespecies despite very modest solubility at physiological pH. MPS1 occupies a central role in mitosis and is one of the main components of the spindle assembly checkpoint. The MPS1 kinase is an attractive cancer target.

References:

1. ARYL SULFONOHYDRAZIDES. WO 2014037750 A1.

2. Introduction of a MethylGroup Curbs Metabolism of Pyrido3, 4- dpyrimidine Monopolar Spindle 1 (MPS1)Inhibitors and Enables the Discovery of the Phase 1 Clinical CandidateN(2)-(2-Ethoxy-4-(4-methyl-4 H-1, 2, 4-triazol-3-yl)phenyl)-6-methyl-N(8)-neopentylpyrido3, 4- dpyrimidine-2, 8-diamine (BOS172722). J Med Chem. 2018Sep 10. doi: 10.1021/acs.jmedchem.8b00690.