DC Chemicals · Product datasheet

Tivozanib(AV-951) — Datasheet

CAT. NO. DC5078

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ParameterValue
Chemical NameTivozanib
CAS No.475108-18-0
SynonymsN-[2-Chloro-4-[(6,7-dimethoxy-4-quinolyl)oxy]phenyl]-N'-(5-methyl-3-isoxazolyl)urea;Tivozanib (AV-951);1-(2-Chloro-4-((6,7-dimethoxyquinolin-4-yl)-oxy)phenyl)-3-(5-methylisoxazol-3-yl)urea;1-(2-Chloro-4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)-3-(5-methylisoxazol-3-yl)urea;1-[2-chloro-4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-3-(5-methyl-1,2-oxazol-3-yl)urea;Av951;AV-951;AV951 Tivozanib;Tivozanib;Tivozanib AV-951;Tivozanib(AV-951,ASP4130,KRN-951);AV951,AV-951;KRN-951;Tivozanib,AV951,AV-951;AV 951;KRN951;KRN 951;1-(2-CHLORO-4-(6,7-DIMETHOXYQUINOLIN-4-YLOXY)PHENYL)-3-(5-METHYLISOXAZOL-3-YL)UREA;172030934T;fotivda;Vascular Endothelial Growth Factor Receptor Tyrosine Kinase Inhibitor IV;N-(2-C
FormulaC22H19ClN4O5
M.Wt454.8631
SMILESClC1C([H])=C(C([H])=C([H])C=1N([H])C(N([H])C1C([H])=C(C([H])([H])[H])ON=1)=O)OC1C([H])=C([H])N=C2C([H])=C(C(=C([H])C2=1)OC([H])([H])[H])OC([H])([H])[H]
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

Tivozanib (AV-951; KRN951) is a highly potent and selective VEGFR 1/2/3 inhibitor with IC50s of 0.21, 0.16, and 0.24 nM in cell assay, respectively.

In Vitro

Tivozanib potently inhibits VEGF-induced VEGFR2 phosphorylation in endothelial cells (IC50=0.16 nM). It also inhibits ligand-induced phosphorylation of PDGFRβ and c-Kit (IC50=1.72 and 1.63 nM, respectively). Tivozanib blocks VEGF-dependent, but not VEGF-independent, activation of mitogenactivated protein kinases and proliferation of endothelial cells. It inhibits VEGF-mediated migration of human umbilical vein endothelial cells[1].

In Vivo

Following p.o. administration to athymic rats, Tivozanib decreases the microvessel density within tumor xenografts and attenuates VEGFR-2 phosphorylation levels in tumor endothelium. It also displays antitumor activity against a wide variety of human tumor xenografts, including lung, breast, colon, ovarian, pancreas, and prostate cancer[1].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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