About: Bcl-2 Inhibitor GDC-0199     Goto   Sponge   NotDistinct   Permalink

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AttributesValues
rdf:type
rdfs:label
  • Bcl-2 Inhibitor GDC-0199
rdfs:subClassOf
Semantic_Type
  • Pharmacologic Substance
Preferred_Name
  • Bcl-2 Inhibitor GDC-0199
NCI_META_CUI
  • CL433816
PDQ_Open_Trial_Search_ID
  • 698675
PDQ_Closed_Trial_Search_ID
  • 698675
FULL_SYN
  • Bcl-2 Inhibitor GDC-0199PTNCI
  • RG7601CNNCI
  • ABT-199CNNCI
  • GDC-0199CNNCI
  • ABT-0199CNNCI
DEFINITION
  • An orally bioavailable, selective small molecule inhibitor of the anti-apoptotic protein Bcl-2, with potential antineoplastic activity. GDC-0199 mimics BH3-only proteins, the native ligands of Bcl-2 and apoptosis activators, by binding to the hydrophobic groove of Bcl-2 proteins thereby repressing Bcl-2 activity and restoring apoptotic processes in tumor cells. Bcl-2 protein is overexpressed in some cancers and plays an important role in the regulation of apoptosis; its expression is associated with increased drug resistance and tumor cell survival. Compared to the Bcl-2 inhibitor navitoclax, this agent does not inhibit bcl-XL and does not cause bcl-XL-mediated thrombocytopenia.NCI
code
  • C103147
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