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AttributesValues
rdf:type
rdfs:label
  • Seliciclib
rdfs:subClassOf
Has_Target
Concept_In_Subset
Semantic_Type
  • Organic Chemical
  • Pharmacologic Substance
Preferred_Name
  • Seliciclib
UMLS_CUI
  • C1436187
CAS_Registry
  • 186692-46-6
FDA_UNII_Code
  • 0ES1C2KQ94
Contributing_Source
  • FDA
PDQ_Open_Trial_Search_ID
  • 511023
PDQ_Closed_Trial_Search_ID
  • 511023
Chemical_Formula
  • C19H26N6O
Legacy_Concept_Name
  • Seliciclib
FULL_SYN
  • R-roscovitineSYNCI
  • CYC202CNNCI
  • SELICICLIBPTFDA0ES1C2KQ94
  • SeliciclibPTNCI
DEFINITION
  • An orally available small molecule and cyclin-dependent kinase (CDK) inhibitor with potential apoptotic and antineoplastic activity. CDKs, serine/threonine kinases that play an important role in cell cycle regulation, are overexpressed in various malignancies. Seliciclib primarily inhibits CDK 2, 7, and 9 by competing for the ATP binding sites on these kinases, leading to a disruption of cell cycle progression. In addition, this agent seems to interfere with CDK-mediated phosphorylation of the carboxy-terminal domain of RNA polymerase II, thereby inhibiting RNA polymerase II-dependent transcription. This may lead to the down-regulation of anti-apoptotic factors, such as myeloid cell leukemia sequence 1 (Mcl-1), a protein crucial for the survival of a range of tumor cell types. The down-regulation of anti-apoptotic factors may lead to an induction of apoptosis, thereby further contributing to seliciclib's antiproliferative effects.NCI
code
  • C62783
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