Chemical Name: N-Methyl-[[3[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]thio]-benzamide
Biological ActivityAxitinib is a potent inhibitor of VEGFR-2, -3, and -1 (IC50 values are 0.2, 0.1-0.3, and 1.2 nM respectively). Exhibits minimal activity against a panel of ~100 protein kinase. Inhibits angiogenesis and vascular permeability. Also a high affinity BCR-ABL1 (T315I) inhibitor (Ki = 149 pM for autophosphorylated ABL1 (T315I)). Blocks proliferation of Ba/F3 cells expressing BCR-ABL1 (T315I). Orally available.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Axitinib effectively inhibits BCR-ABL1(T315I) with a distinct binding conformation.
Pemovska et al.
Nonclinical antiangiogenesis and antitumor activities of axitinib (AG-013736), an oral, potent, and selective inhibitor of vascular endothelial growth factor receptor tyrosine kinases 1, 2 and 3.
Hu-Lowe et al.
Clin.Cancer Res., 2008;14:7272
Modulation of the antitumor activity of metronomic cyclophosph. by the angiogenesis inhibitor axitinib.
Ma and Waxman
Mol.Cancer Ther., 2008;7:79
Citations for Axitinib
The citations listed below are publications that use Tocris products. Selected citations for Axitinib include:
3 Citations: Showing 1 - 3
Superantigens are critical for Staphylococcus aureus Infective endocarditis, sepsis, and acute kidney injury.
Authors: Salgado-Pabón Et al.
Lenticular cytoprotection. Part 1: the role of hypoxia inducible factors-1α and -2α and vascular endothelial growth factor in lens epithelial cell survival in hypoxia.
Authors: Neelam Et al.
Mol Vis 2013;19:1
Magnetic nanoparticle-mediated massively parallel mechanical modulation of single-cell behavior.
Authors: Tseng Et al.
Sci Rep 2012;9:1113
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