Axitinib

Cat. No. 4350

Axitinib C22H18N4OS [319460-85-0]

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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.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Pemovska et al (2015) Axitinib effectively inhibits BCR-ABL1(T315I) with a distinct binding conformation. Nature 519 102. PMID: 25686603.

Hu-Lowe et al (2008) 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. Clin.Cancer Res. 14 7272. PMID: 19010843.

Ma and Waxman (2008) Modulation of the antitumor activity of metronomic cyclophosphamide by the angiogenesis inhibitor axitinib. Mol.Cancer Ther. 7 79. PMID: 18202011.

If you know of a relevant reference for Axitinib please let us know.

Citations are publications that use Tocris products. Selected citations for Axitinib include:

Salgado-Pabón et al (2013) Superantigens are critical for Staphylococcus aureus Infective endocarditis, sepsis, and acute kidney injury. MBio 4. PMID: 23963178.

Tseng et al (2012) Magnetic nanoparticle-mediated massively parallel mechanical modulation of single-cell behavior. Sci Rep 9 1113. PMID: 23064517.

Do you know of a great paper that uses Axitinib from Tocris? If so please let us know.

View Related Products by Product Action

Keywords: Axitinib, supplier, Axitinib, inhibits, VEGFR-1, VEGFR-2, VEGFR-3, inhibitors, VEGF, receptor, receptors, vascular, endothelial, growth, factor, BCR-ABL, Tocris Bioscience, VEGFR Inhibitor products

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