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.
Compound Libraries
Axitinib is also offered as part of the Tocriscreen Plus, Tocriscreen Kinase Inhibitor Toolbox II and Tocriscreen Library of FDA-Approved Compounds. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 386.47 |
| Formula | C22H18N4OS |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 319460-85-0 |
| PubChem ID | 6450551 |
| InChI Key | RITAVMQDGBJQJZ-FMIVXFBMSA-N |
| Smiles | O=C(NC)C1=C(SC2=CC=C(C(/C=C/C4=CC=CC=N4)=NN3)C3=C2)C=CC=C1 |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 9.66 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 386.47. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.59 mL | 12.94 mL | 25.88 mL |
| 5 mM | 0.52 mL | 2.59 mL | 5.18 mL |
| 10 mM | 0.26 mL | 1.29 mL | 2.59 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
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References
References are publications that support the products' biological activity.
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
Pemovska et al (2015) Axitinib effectively inhibits BCR-ABL1(T315I) with a distinct binding conformation. Nature 519 102 PMID: 25686603
Keywords: Axitinib, supplier, Axitinib, inhibits, VEGFR-1, VEGFR-2, VEGFR-3, inhibitors, VEGF, receptor, receptors, vascular, endothelial, growth, factor, BCR-ABL, VEGFR, VEGFR, Tocris Bioscience
