Axitinib

Biological Activity

Axitinib is a potent inhibitor of VEGFR-2, -3, and -1 (IC₅₀ values are 0.2, 0.1-0.3, and 1.2 nM respectively). Axitinib exhibits minimal activity against a panel of ~100 protein kinases. Axitinib inhibits angiogenesis and vascular permeability. Also a high affinity BCR-ABL1 (T315I) inhibitor (K_i = 149 pM for autophosphorylated ABL1 (T315I)). Axitinib blocks proliferation of Ba/F3 cells expressing BCR-ABL1 (T315I). Axitinib (10 mg/kg) decreases T-cell exhaustion and tumor and T-cell hypoxia and improves survival in mice in vivo. Orally available.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Background References

1. Axitinib effectively inhibits BCR-ABL1(T315I) with a distinct binding conformation.
   Pemovska et al.
   Nature, 2015;519:102
2. 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
3. Modulation of the antitumor activity of metronomic cyclophosph. by the angiogenesis inhibitor axitinib.
   Ma and Waxman
   Mol.Cancer Ther., 2008;7:79

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