Axitinib

Name: Axitinib
Brand: Tocris Bioscience
SKU: 4350

Tocris Bioscience, part of Bio-Techne | Catalog # 4350

Citations (15)

COA / SDS

Potent VEGFR-1, -2 and -3 inhibitor

Key Product Details

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)
Molecular Weight:	386.47

View Full Technical Details for Axitinib

Technical Data
Citations

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 (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.

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 for Axitinib

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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	103.50 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

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References for Axitinib

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