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Version: 17.12d (Release date: 2017-12-26)
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CDKI R547 (Code C64544)

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Terms & Properties

Preferred Name: CDKI R547

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.

Label: CDKI R547

NCI Thesaurus Code: C64544 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C1832011  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
Cyclin Dependent Kinase Inhibitor R547
Cyclin-Dependent Kinase Inhibitor R547

External Source Codes: 
PDQ Closed Trial Search ID 529189
PDQ Open Trial Search ID 529189 (check for NCI PDQ open clinical trial info)
UMLS CUI C1832011

Other Properties:
     Name Value (qualifiers indented underneath)
code C64544
Legacy_Concept_Name R547
Semantic_Type Organic Chemical
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  


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