Preferred Label : Checkpoint Kinase Inhibitor XL844;
NCIt synonyms : Chk Inhibitor XL844;
NCIt 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.;
Molecule name : XL844;
PubMed : 20024691;
Origin ID : C61102;
UMLS CUI : C1831757;
Semantic type(s)
- concept_is_in_subset
- has_target
