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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.
Sold for research purposes under agreement from Pfizer Inc.
Compound Libraries for Axitinib
Technical Data for Axitinib
|Storage||Store at +4°C|
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|
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|
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
3 Citations for Axitinib
Citations are publications that use Tocris products. Selected citations for Axitinib include:
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
Tseng et al (2012) Magnetic nanoparticle-mediated massively parallel mechanical modulation of single-cell behavior. Sci Rep 9 1113 PMID: 23064517
Salgado-Pabón et al (2013) Superantigens are critical for Staphylococcus aureus Infective endocarditis, sepsis, and acute kidney injury. MBio 4 PMID: 23963178
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Reviews for Axitinib
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Literature in this Area
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