Catalog Number: 4350
Chemical Name: N-Methyl-[[3[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]thio]-benzamide
Biological Activity
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.
Technical Data
  • M.Wt:
    386.47
  • Formula:
    C22H18N4OS
  • Solubility:
    Soluble to 25 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at +4°C
  • CAS No:
    319460-85-0
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from Pfizer Inc.
Background References
  1. Modulation of the antitumor activity of metronomic cyclophosphamide by the angiogenesis inhibitor axitinib.
    Ma and Waxman
    Mol.Cancer Ther., 2008;7:79
  2. Axitinib effectively inhibits BCR-ABL1(T315I) with a distinct binding conformation.
    Pemovska et al.
    Nature, 2015;519:102
  3. 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
Citations:

The citations listed below are publications that use Tocris products. Selected citations for Axitinib include:

2 Citations: Showing 1 - 2
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  1. Superantigens are critical for Staphylococcus aureus Infective endocarditis, sepsis, and acute kidney injury.
    Authors: Salgado-Pabón Et al.
    MBio 2013;4
  2. Magnetic nanoparticle-mediated massively parallel mechanical modulation of single-cell behavior.
    Authors: Tseng Et al.
    Sci Rep 2012;9:1113

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