About: Checkpoint Kinase Inhibitor XL844     Goto   Sponge   NotDistinct   Permalink

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AttributesValues
rdf:type
rdfs:label
  • Checkpoint Kinase Inhibitor XL844
rdfs:subClassOf
Semantic_Type
  • Organic Chemical
  • Pharmacologic Substance
Preferred_Name
  • Checkpoint Kinase Inhibitor XL844
PubMedID_Primary_Reference
  • 20024691
UMLS_CUI
  • C1831757
PDQ_Open_Trial_Search_ID
  • 469731
PDQ_Closed_Trial_Search_ID
  • 469731
Legacy_Concept_Name
  • XL844
FULL_SYN
  • Checkpoint Kinase Inhibitor XL844PTNCI
  • XL844CNNCI
  • Chk Inhibitor XL844SYNCI
DEFINITION
  • A synthetic small-molecule inhibitor of checkpoint kinases 1 and 2 (Chk1 and Chk2) with potential antineoplastic activity. XL844 binds to and inhibits Chks 1 and 2, resulting in inhibition of cell cycle arrest, progressive DNA damage, inhibition of DNA repair, and, ultimately, tumor cell apoptosis. This agent also inhibits vascular endothelial growth factor receptor 1 (VEGFR1) and vascular endothelial growth factor receptor 3 (VEGFR3), important mediators of tumor angiogenesis and lymphogenesis, respectively. In the presence of extensive damage or absence of timely repair, these checkpoint-signaling pathways may also trigger a pathway that effects apoptosis. Normal functions of Chks involve the initiation of cell-cycle arrest and the up-regulation of transcription genes involved with DNA excision repair and dNTP synthesis.NCI
code
  • C61102
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