Preferred Label : Empesertib;
NCIt synonyms : (2R)-2-(4-Fluorophenyl)-N-(4-(2-((2-methoxy-4-(methylsulfonyl)phenyl)amino)(1,2,4)triazolo(1,5-a)pyridin-6-yl)phenyl)propanamide;
NCIt definition : An orally bioavailable, selective inhibitor of the serine/threonine monopolar spindle
1 (Mps1) kinase, with potential antineoplastic activity. Upon administration, empesertib
binds to and inhibits the activity of Mps1. This 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. Mps1,
a kinase expressed in proliferating normal tissues and aberrantly overexpressed in
a wide range of human tumors, is activated during mitosis and is essential for SAC
functioning and controls chromosome alignment.;
UNII : 02Y3Z2756M;
InChIKey : NRJKIOCCERLIDG-GOSISDBHSA-N;
CAS number : 1443763-60-7;
Molecule name : BAY116-1909;
NCI Metathesaurus CUI : CL473492;
Origin ID : C116074;
UMLS CUI : C4682398;
Semantic type(s)
- concept_is_in_subset
