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AttributesValues
rdf:type
rdfs:label
  • CDKI R547
rdfs:subClassOf
Has_Target
Semantic_Type
  • Organic Chemical
  • Pharmacologic Substance
Preferred_Name
  • CDKI R547
UMLS_CUI
  • C1832011
PDQ_Open_Trial_Search_ID
  • 529189
PDQ_Closed_Trial_Search_ID
  • 529189
Legacy_Concept_Name
  • R547
FULL_SYN
  • R547CNNCI
  • Cyclin Dependent Kinase Inhibitor R547SYNCI
  • Cyclin-Dependent Kinase Inhibitor R547SYNCI
  • CDKI R547PTNCI
DEFINITION
  • An orally bioavailable diaminopyrimidine compound and a cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. CDKs are ATP-dependent serine/threonine kinases that are important regulators of cell cycle progression and are frequently overexpressed in cancerous cells. R547 selectively binds to and inhibits CDKs, especially CDK1/cyclin B, CDK2/cyclin E, and CDK4/cyclin D1. The inhibition of CDKs results in cell cycle arrest, inhibition of tumor cell proliferation, and induction of apoptosis. By inhibiting CDK activity, R547 also reduces phosphorylation of the retinoblastoma (Rb) protein, thereby preventing activation of transcription factor E2F and leading to further suppression of tumor cell proliferation.NCI
code
  • C64544
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