Axitinib

Pricing Availability Delivery Time Qty
Cat.No. 4350 - Axitinib | C22H18N4OS | CAS No. 319460-85-0
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)
Datasheet
Citations (2)
Literature
Pathways

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.

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

Molarity Calculator

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Reconstitution Calculator

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Product Datasheets

Safety Datasheet

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


If you know of a relevant reference for Axitinib, please let us know.

View Related Products by Product Action

View all VEGFR Inhibitors

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

2 Citations for Axitinib

Citations are publications that use Tocris products. Selected citations for Axitinib include:

Salgado-Pabón et al (2013) Superantigens are critical for Staphylococcus aureus Infective endocarditis, sepsis, and acute kidney injury. MBio 4 PMID: 23963178

Tseng et al (2012) Magnetic nanoparticle-mediated massively parallel mechanical modulation of single-cell behavior. Sci Rep 9 1113 PMID: 23064517


Do you know of a great paper that uses Axitinib from Tocris? If so please let us know.

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Reviews

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Angiogenesis in Cancer

Angiogenesis in Cancer Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Pathways for Axitinib

VEGF

VEGF Signaling Pathway

VEGF signaling pathway is involved in embryonic vascular development (vasculogenesis) and in the formation of new blood vessel (angiogenesis). It also induces cell migration, proliferation and survival.

Protocols

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