Information BAY 1217389 BAY 1217389 is an orally bioavailable, selective inhibitor of the serine/threonine kinase monopolar spindle 1 (Mps1) with IC50 values below 10 nmol/L while showing an excellent selectivity profile. Targets Mps1 (Cell-free assay) 0.63 nM In vitro In biochemical assays, the IC50 value of BAY 1217389 is 0.63±0.27 nmol/L. It shows high selectivity against other kinases and found to bind to PDGFRβ ( 300 nmol/L). In vivo BAY 1217389 achieves moderate efficacy in monotherapy in tumor xenograft studies. Its blood clearance is found to be low in the tested species. Vss is high and terminal half-lives were long. BAY 1217389 is administered orally to female NMRI mouse (1 mg/kg) and male Wistar rat (0.5 mg/kg). Peak plasma concentrations are observed between 1.5 and 7 hours. Oral bioavailability is high in rat and moderate in mouse. Cell Research(from reference) Cell lines：Tumor cell lines HeLa-MaTu and HeLa-MaTu-ADR cells Incubation Time：96 h
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BAY 1217389
CAS number：1554458-53-5 molecular formula：C27H24F5N5O3
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| Chinese alias | - | ||
| English alias | AKOS032944938 | AC-36064 | HY-12859 | NSC787026 | NSC-787026 | BAY1217389 | BAY-1217389 | GTPL12705 | M964LB1114 | EX-A948 | J-690208 | N-cyclopropyl-4-[6-(2,3-difluoro-4-methoxyphenoxy)-8-[(3,3,3-trifluoropropyl)amino]imidazo[1,2-b]pyridazin-3-yl]-2-meth | ||
| CAS number | 1554458-53-5 | molecular formula | C27H24F5N5O3 |
| molecular weight | 561.50 g/mol | Exact mass | 10mM in DMSO |
| PSA | 89.800 Ų | logp | 5.7 |
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