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 <1 nM. Empesertib has potential antineoplastic activity.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Dual specificity protein kinase TTK inhibitor
Product Description
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 <1 nM. Empesertib has potential antineoplastic activity.
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.
C2429551