CEP-11981

  • Chemical Properties
CAS No. 856691-93-5 Cat. No. BCP46664
Name CEP-11981
Synonyms CEP11981; CEP 11981; BOL303213X; BOL-303213X; BOL 303213X; ESK981; ESK-981; ESK 981;
Formula C28H27N7O M. Wt 477.56
  • Biological Activity
Description CEP-11981 is a potent orally active inhibitor of multiple targets (TIE-2, VEGF-R1, 2, and 3, and FGF-R1), which having essential and nonredundant roles in tumor angiogenesis and vascular maintenance. CEP-11981 demonstrated significant preclinical cytostatic anti-tumor activity against human UC xenografts in a murine model, which was attributable to inhibition of angiogenesis. Clinical development of CEP-11981 in tolerable combination regimens and the discovery of tumor and host related biomarkers predictive for benefit are warranted. Pan-VEGFR/Tie2 tyrosine kinase inhibitor CEP-11981 selectively binds to VEGFR and Tie2 receptor tyrosine kinases, which may result the inhibition of endothelial cell migration, proliferation and survival and the inhibition of tumor cell proliferation and tumor cell death.
Pathways Angiogenesis/Protein Tyrosine Kinase 
Targets VEGFR 

Structure

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