Empesertib (BAY-1161909)

Description: Empesertib (also known as BAY 1161909) is a novel, potent, orally bioavailable, and selective inhibitor of serine/threonine kinase Mps1 (monopolar spindle 1) with an IC50 of < 1 nM. Empesertib has potential antineoplastic activity, it binds to and inhibits the activity of Mps1 which causes inactivation of the spindle assembly checkpoint (SAC), accelerated mitosis, chromosomal misalignment, chromosomal missegregation, mitotic checkpoint complex destabilization, and increased aneuploidy. This leads to the induction of cell death in cancer cells overexpressing Mps1.