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Version: 17.10e (Release date: 2017-10-30)
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Checkpoint Kinase Inhibitor XL844 (Code C61102)

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Terms & Properties

Preferred Name: Checkpoint Kinase Inhibitor XL844

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.

Display Name: Checkpoint Kinase Inhibitor XL844

Label: Checkpoint Kinase Inhibitor XL844

NCI Thesaurus Code: C61102 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C1831757  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
Checkpoint Kinase Inhibitor XL844
Chk Inhibitor XL844

External Source Codes: 
PDQ Closed Trial Search ID 469731
PDQ Open Trial Search ID 469731 (check for NCI PDQ open clinical trial info)
PubMedID Primary Reference 20024691 (see PubMed Primary Reference info)
UMLS CUI C1831757

Other Properties:
     Name Value (qualifiers indented underneath)
code C61102
Contributing_Source CTRP
Legacy_Concept_Name XL844
Semantic_Type Organic Chemical
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  


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