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Submit ReviewAxitinib
Description: Potent VEGFR-1, -2 and -3 inhibitor
Chemical Name: N-Methyl-[[3[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]thio]-benzamide
Purity: ≥99% (HPLC)
Biological Activity for Axitinib
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 (Ki = 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.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Compound Libraries for Axitinib
Axitinib is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.
Technical Data for Axitinib
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Axitinib
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 9.66 | 25 |
Preparing Stock Solutions for Axitinib
The following data is based on the product molecular weight 386.47. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.25 mM | 10.35 mL | 51.75 mL | 103.5 mL |
| 1.25 mM | 2.07 mL | 10.35 mL | 20.7 mL |
| 2.5 mM | 1.04 mL | 5.18 mL | 10.35 mL |
| 12.5 mM | 0.21 mL | 1.04 mL | 2.07 mL |
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Product Datasheets for Axitinib
References for Axitinib
References are publications that support the biological activity of the product.
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 cyclophosph. 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
Scharping (2021) Mitochondrial stress induced by continuous stimulation under hypoxia rapidly drives T cell exhaustion. Nat.Immunol. 22 205 PMID: 33398183
If you know of a relevant reference for Axitinib, please let us know.
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Keywords: Axitinib, Axitinib supplier, Axitinib, inhibits, VEGFR-1, VEGFR-2, VEGFR-3, inhibitors, VEGF, receptor, receptors, vascular, endothelial, growth, factor, BCR-ABL, VEGFR, 4350, Tocris Bioscience
5 Citations for Axitinib
Citations are publications that use Tocris products. Selected citations for Axitinib include:
Tseng et al (2012) Magnetic nanoparticle-mediated massively parallel mechanical modulation of single-cell behavior. Sci Rep 9 1113 PMID: 23064517
Neelam et al (2013) 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. Mol Vis 19 1 PMID: 23335846
Andrea et al (2015) VEGF and LPS synergistically silence inflammatory response to Plasmodium berghei infection and protect against cerebral malaria. Pathog Glob Health 109 255-65 PMID: 26392042
Jung Yoon et al (2022) The Potential of Transforming Growth Factor-beta Inhibitor and Vascular Endothelial Growth Factor Inhibitor as Therapeutic Agents for Uterine Leiomyoma. Int J Med Sci 19 1779-1786 PMID: 36313223
Salgado-Pabón et al (2013) Superantigens are critical for Staphylococcus aureus Infective endocarditis, sepsis, and acute kidney injury. MBio 4 PMID: 23963178
Do you know of a great paper that uses Axitinib from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Angiogenesis in Cancer Poster
This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.
Pathways for Axitinib
