Preferred Label : Trilaciclib;
NCIt synonyms : Spiro(cyclohexane-1,9'(6'H)-pyrazino(1',2':1,5)pyrrolo(2,3-d)pyrimidin)-6'-one, 7',8'-dihydro-2'-((5-(4-methyl-1-piperazinyl)-2-pyridinyl)amino)-; 2'-((5-(4-Methylpiperazin-1-yl)pyridin-2-yl)amino)-7',8'-dihydro-6'H-spiro(cyclohexane-1,9'-pyrazino(1',2':1,5)pyrrolo(2,3-d)pyrimidin)-6'-one;
NCIt definition : A small molecule, competitive inhibitor of cyclin dependent kinases 4 and 6 (CDK4/6),
with potential antineoplastic and chemoprotective activities. Upon intravenous administration,
trilaciclib binds to and inhibits the activity of CDK4/6, thereby blocking the phosphorylation
of the retinoblastoma protein (Rb) in early G1. This prevents G1/S phase transition,
causes cell cycle arrest in the G1 phase, induces apoptosis, and inhibits the proliferation
of CDK4/6-overexpressing tumor cells. In patients with CDK4/6-independent tumor cells,
G1T28 may protect against multi-lineage chemotherapy-induced myelosuppression (CIM)
by transiently and reversibly inducing G1 cell cycle arrest in hematopoietic stem
and progenitor cells (HSPCs) and preventing transition to the S phase. This protects
all hematopoietic lineages, including red blood cells, platelets, neutrophils and
lymphocytes, from the DNA-damaging effects of certain chemotherapeutics and preserves
the function of the bone marrow and the immune system. CDKs are serine/threonine kinases
involved in the regulation of the cell cycle and may be overexpressed in certain cancer
cell types. HSPCs are dependent upon CDK4/6 for proliferation.;
UNII : U6072DO9XG;
InChIKey : PDGKHKMBHVFCMG-UHFFFAOYSA-N;
CAS number : 1374743-00-6;
Molecule name : G1T28;
Origin ID : C123281;
UMLS CUI : C4524320;
Automatic exact mappings (from CISMeF team)
- Currated CISMeF NLP mapping
- See also inter- (CISMeF)
- Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
- has_target
