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Cat. No. Name Size Price Add Cart
KI0652CEP-7055QuoteQuote

Chemical Characteristic

Product NameCEP-7055
CAS No.402857-58-3
Molecular Weight 525.26
FormulaC32H35N3O4
Chemical NameGlycine, N,N-dimethyl-,3-[5,6,7,13-tetrahydro-9-[(1-methylethoxy)methyl]-5-oxo-12H-indeno[2,1-a]pyrrolo[3,4-c]carbazol-12-yl]propylester
SmilesC(=O)(CN(C)C)OCCCn1c2c3c(c4c(c2c2cc(ccc12)COC(C)C)CNC4=O)c1c(C3)cccc1
Chemical Structure

Biological activities

CEP-7055 is a fully synthetic orally active pan-VEGF-R kinase inhibitor. CEP-7055 is the prodrug of CEP-5214. In biochemical kinase assays, the IC50 values of CEP-5214 is 18, 12, and 17 nM against human VEGF-R2/KDR kinase, VEGF-R1/FLT-1 kinase, and VEGF-R3/FLT-4 kinase, respectively.[1] In vivo, chronic co-administration of CEP-7055 (23.8 mg/kg/dose) and temozolomide results in improvement of median survival of nude mice bearing orthotopic human glioblastoma xenografts compared with temozolomide alone. CEP-7055 administration alone also reduces neurologic dysfunction, brain edema, hemorrhage, and intratumoral microvessel density (CD34 staining) in glioma-bearing mice. Furthermore, the administration of CEP-7055 in combination with irinotecan and to a lesser degree with oxaliplatin shows reductions on primary colon carcinoma and hepatic metastatic burden in the CT-26 tumor model relative to that achieved by irinotecan and oxaliplatin monotherapy.[2] Administration p.o. of CEP-7055 (2.57 to 23.8 mg/kg/dose b.i.d.) results in dose-related reductions in neovascularization in vivo in porcine aortic endothelial cell (PAEC)-VEGF/basic fibroblast growth factor-Matrigel implants in nude mice. Administration p.o. of CEP-7055 (2.57 to 23.8 mg/kg/dose b.i.d.) results in 30% reduction in granuloma formation and 42% reduction granuloma vascularity in a murine chronic inflammation-induced angiogenesis model. Administration p.o. of CEP-7055 (2.57 to 23.8 mg/kg/dose b.i.d.) also results in significant and sustained inhibition of VEGF-induced plasma extravasation in rats, with an ED50 of 20 mg/kg/dose.[1]

References

[1] Jones-Bolin S, et al. The effects of the oral, pan-VEGF-R kinase inhibitor CEP-7055 and chemotherapy in orthotopic models of glioblastoma and colon carcinoma in mice. Mol Cancer Ther. 2006, 5(7): 1744-1753.
[2] Ruggeri B, et al. CEP-7055: a novel, orally active pan inhibitor of vascular endothelial growth factor receptor tyrosine kinases with potent antiangiogenic activity and antitumor efficacy in preclinical models. Cancer Res. 2003, 63(18): 5978-5991.

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