CEP-11981 - CAS 856691-93-5
Catalog number:
856691-93-5
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
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Description:
CEP-11981 is an orally bioavailable inhibitor of vascular endothelial growth factor receptor (VEGFR) and Tie2 receptor tyrosine kinases with potential antiangiogenic and antineoplastic activities. 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. VEGFR and Tie2 are frequently overexpressed by a variety of tumor cell types and play crucial roles in the regulation of angiogenesis and the maintenance of tumor blood vessels. Tie2 (tyrosine kinase with immunoglobulin-like and EGF-like domains) is activated by angiopoietin-1 (Ang-1).
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Appearance:
Solid powder
Synonyms:
CEP-11981; CEP 11981; CEP11981
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Current Developer:
Cephalon, Inc
1.Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidi
Hudkins RL1, Becknell NC, Zulli AL, Underiner TL, Angeles TS, Aimone LD, Albom MS, Chang H, Miknyoczki SJ, Hunter K, Jones-Bolin S, Zhao H, Bacon ER, Mallamo JP, Ator MA, Ruggeri BA. J Med Chem. 2012 Jan 26;55(2):903-13. doi: 10.1021/jm201449n. Epub 2012 Jan 6.
A substantial body of evidence supports the utility of antiangiogenesis inhibitors as a strategy to block or attenuate tumor-induced angiogenesis and inhibition of primary and metastatic tumor growth in a variety of solid and hematopoietic tumors. Given the requirement of tumors for different cytokine and growth factors at distinct stages of their growth and dissemination, optimal antiangiogenic therapy necessitates inhibition of multiple, complementary, and nonredundant angiogenic targets. 11-(2-Methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (11b, CEP-11981) is a potent orally active inhibitor of multiple targets (TIE-2, VEGF-R1, 2, and 3, and FGF-R1) having essential and nonredundant roles in tumor angiogenesis and vascular maintenance. Outlined in this article are the design strategy, synthesis, and biochemical and pharmacological profile for 11b, which completed Phase I clinical assessing safety and pharmacokinetics allowing for the initiation of proof of concept studies.
2.An open-label study to determine the maximum tolerated dose of the multitargeted tyrosine kinase inhibitor CEP-11981 in patients with advanced cancer.
Pili R1, Carducci M, Brown P, Hurwitz H. Invest New Drugs. 2014 Dec;32(6):1258-68. doi: 10.1007/s10637-014-0147-9. Epub 2014 Aug 26.
BACKGROUND: This phase I study evaluated the pharmacokinetics and pharmacodynamics of CEP-11981, an oral vascular endothelial growth factor (VEGF) tyrosine kinase inhibitor, in patients with advanced, relapsed, or refractory solid tumors.
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CAS 856691-93-5 CEP-11981

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