CDK Inhibitor R547

Preferred Label : CDK Inhibitor R547;

NCIt synonyms : Cyclin-Dependent Kinase Inhibitor R547; Cyclin Dependent Kinase Inhibitor R547;

NCIt related terms : R-547;

NCIt 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.;

UNII : T61871RKRI;

InChIKey : JRNJNYBQQYBCLE-UHFFFAOYSA-N;

CAS number : 741713-40-6;

Molecule name : R547; RO-4584820; RO 4584820; R 547;

Details

Origin ID

C64544;

UMLS CUI

C1832011;

Semantic type(s)
- Organic Chemical [UMLS semantic type]
- Pharmacologic Substance [UMLS semantic type]
chemical_or_drug_affects_gene_product
- Cyclin-Dependent Kinase [NCIt concept]
chemical_or_drug_has_mechanism_of_action
- Enzyme Inhibition [NCIt concept]
chemical_or_drug_has_physiologic_effect
- Negative Regulation of G1 Phase [NCIt concept]
- Negative Regulation of G2 to M Transition [NCIt concept]
- Positive Regulation of Apoptosis [NCIt concept]
- Protein Phosphorylation Inhibition [NCIt concept]
concept_is_in_subset
- FDA Established Names and Unique Ingredient Identifier Codes Terminology [NCIt concept]
- GDC Terminology [NCIt concept]
- GDC Therapeutic Agent Terminology [NCIt concept]
- GDC Value Terminology [NCIt concept]
- NCI Drug Dictionary Terminology [NCIt concept]
- NCIt Antineoplastic Agent Terminology [NCIt concept]
has_target
- Cyclin-Dependent Kinase 1 [NCIt concept]
- Cyclin-Dependent Kinase 2 [NCIt concept]
- Cyclin-Dependent Kinase 4 [NCIt concept]

Keyword's position in hierarchy(ies) :

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