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Biological Activity:
A highly potent and orally available tyrosine kinase inhibitor (TKI), targeting VEGFR-1, 2 and 3, c-KIT and PDGFR (IC50: 0.21, 0.16, 0.24, 1.63 and 1.72 nM, respectively).
References:
K Nakamura 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. [online]
Eri Taguchi 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. [online]
C Campas et al. Tivozanib. Drugs Fut. 2009, 34(10), 793. [online]
Chemical Name: 1-(2-chloro-4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)-3-(5-methylisoxazol-3-yl)urea
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