BOS172722 is a monopolar spindle 1 (MPS1) checkpoint inhibitor with IC50 of 11 nM, Ki of 0.11 nM.
BOS172722 optimizes HLM stability, CDK2 selectivity, cellular potency, and solubility. BOS172722 is potential for the treatment of various forms of breast cancer.[1]
BOS172722 shows excellent PK in mouse, rat, and dog. At 1 mg/kg iv and 5 mg/kg po, BOS172722 shows complete bioavailability (100%), low clearance (1.2 mL/min/kg), a moderate volume of distribution (1.1 L/kg), and a 12 h half-life in a dog PK study. The 50 mg/kg dose of BOS172722 results in an increased suppression of MPS1 autophosphorylation at 6 and 24 h.[1]
[1] Hannah L Woodward, et al. J Med Chem. 2018 Sep 27;61(18):8226-8240.