Information Empesertib (BAY1161909) Empesertib (BAY1161909, Mps1-IN-5), a derivative of triazolopyridine, is an orally bioavailable, selective inhibitor of the serine/threonine monopolar spindle 1 (Mps1) kinase with IC50 of Targets Mps1 (Cell-free assay) 1 nM In vitro Empesertib (BAY1161909) is a very effective Mps-1 inhibitor with an IC50 lower than or equal to 1 nM (more potent than 1 nM) in an Mps-1 kinase assay with a concentration of 1 μM/2 mM ATP, and an IC50 lower than 400 nM in a HeLa cell proliferation assay. In vivo Empesertib (BAY1161909) is a very effective Mps-1 inhibitor with a maximum oral bioavailability (Fmax) in rat that is higher than 70%, determined by means of rat liver microsomes, and a maximum oral bioavailability (Fmax) in dog that is higher than 50%, determined by means of dog liver microsomes, and a maximum oral bioavailability (Fmax) in human that is higher than 60%, determined by means of human liver microsomes. Cell Research(from reference) Cell lines：Cultivated tumor cells Concentrations：0.01 μM-30 μM Incubation Time：4 days
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Empesertib (BAY1161909)
CAS number：1443763-60-7 molecular formula：C29H26FN5O4S
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| Chinese alias | - | ||
| English alias | A908652 | (-)-BAY-1161909 | Benzeneacetamide, 4-fluoro-N-[4-[2-[[2-methoxy-4-(methylsulfonyl)phenyl]amino][1,2,4]triazolo[1,5-a] | (2R)-2-(4-fluorophenyl)-N-[4-(2-{[2-methoxy-4-(methylsulfonyl)phenyl]amino}[1,2,4]triazolo[1,5-alpha]pyridin-6-yl)phenyl]pro | ||
| CAS number | 1443763-60-7 | molecular formula | C29H26FN5O4S |
| molecular weight | 559.61 g/mol | Exact mass | - |
| PSA | 123.000 Ų | logp | 4.9 |
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