Axitinib

Product Description

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.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.25 mM	10.35 mL	51.75 mL	103.50 mL
1.25 mM	2.07 mL	10.35 mL	20.70 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

Calculators

Background References

References are publications that support the biological activity of the product.

• Scharping Mitochondrial stress induced by continuous stimulation under hypoxia rapidly drives T cell exhaustion. Nat.Immunol. 2021 PMID: 33398183
• Ma and Waxman Modulation of the antitumor activity of metronomic cyclophosph. by the angiogenesis inhibitor axitinib. Mol.Cancer Ther. 2008 PMID: 18202011
• Pemovska Axitinib effectively inhibits BCR-ABL1(T315I) with a distinct binding conformation. Nature 2015 PMID: 25686603
• Hu-Lowe 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. 2008 PMID: 19010843