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Cat. No. Name Size Price Add Cart
KI0078Tivozanib5 mg$192
Tivozanib10 mg$272
Tivozanib50 mg$912

Chemical Characteristic

Product NameTivozanib
SynonymsAV-951, KRN-951
CAS No.475108-18-0
Molecular Weight 454.86
FormulaC22H19ClN4O5
Chemical Name1-(2-chloro-4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-3-(5-methylisoxazol-3-yl)urea
SmilesN(C(=O)Nc1noc(c1)C)c1c(cc(cc1)Oc1ccnc2c1cc(c(c2)OC)OC)Cl
Chemical Structure

Biological activities

Tivozanib is a highly potent inhibitor of vascular endothelial growth factor receptor (VEGFR) tyrosine kinases. The IC50 of tivozanib is 0.16, 0.21 and 0.24 nM against VEGFR-2, VEGFR-1 and VEGFR-3, respectively. In addition, tivozanib also inhibits ligand-induced phosphorylation of platelet-derived growth factor receptor-β (PDGFR-β) and c-Kit with an IC50 of 1.72 and 1.63 nM, respectively. Tivozanib blocks VEGF-dependent, but not VEGF-independent, activation of mitogen-activated protein kinases and proliferation of endothelial cells. In addition, tivozanib inhibits VEGF-mediated migration of human umbilical vein endothelial cells.[1] Following p.o. administration to athymic rats, tivozanib decreases the microvessel density within tumor xenografts and attenuates VEGFR-2 phosphorylation levels in tumor endothelium. Tivozanib also displays antitumor activity against a wide variety of human tumor xenografts, including lung, breast, colon, ovarian, pancreas, and prostate cancer.[1] It is also reported that tivozanib produces a significant inhibition of tumor growth and angiogenesis in athymic rats.[2] Tivozanib treatments that commences 4 days after tumor transplantation (day 4) significantly inhibits tumor-induced angiogenesis, the formation of tumor nodules in the mesenteric windows, and the accumulation of malignant ascites. Moreover, tivozanib treatments initiates on day 14, by which time angiogenesis and malignant ascites have already been well established, results in the regression of newly formed tumor vasculatures with aberrant structures.[3]

References

[1] Nakamura K, et al. KRN951, a highly potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, has antitumor activities and affects functional vascular properties. Cancer Res. 2006, 66(18): 9134-9142.
[2] De Luca A, et al. Tivozanib, a pan-VEGFR tyrosine kinase inhibitor for the potential treatment of solid tumors. IDrugs. 2010, 13(9): 636-645.
[3] Taguchi E, et al. Anti-tumor activity and tumor vessel normalization by the vascular endothelial growth factor receptor tyrosine kinase inhibitor KRN951 in a rat peritoneal disseminated tumor model. Cancer Sci. 2008, 99(3): 623-630.

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