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Axitinib (AG 013736) (Synonyms: AG 013736)

Catalog No.GC12216

Axitinib (AG 013736) is a multi-targeted tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively.

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Axitinib (AG 013736) Chemical Structure

Cas No.: 319460-85-0

Size Price Stock Qty
10mM (in 1mL DMSO)
$40.00
In stock
50mg
$35.00
In stock
100mg
$64.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

PAE cells overexpressing RTK, Human umbilical vein endothelial cells (HUVEC)

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

Cellular receptor kinase phosphorylation assay: 45 min at 37 ℃ in the presence of 1 mmol/L Na3VO4

Applications

In transfected or endogenous RTK-expressing cells, axitinib potently blocked growth factor-stimulated phosphorylation of VEGFR-2 and VEGFR-3 with average IC50 values of 0.2 and 0.1 to 0.3 nmol/L, respectively. Axitinib inhibited VEGF-stimulated survival of HUVEC with IC50 value of 0.17 nmol/L.

Animal experiment [2]:

Animal models

Female nu/nu mice or severe combined immunodeficient beige mice(ages 7-10 weeks)

Dosage form

Axitinib was dosed as a suspension at 5 mL/kg orally twice daily

Applications

Axitinib dose-dependently inhibits tumor growth in MV522 with ED50 value of 8.8 mg/kg twice daily, based on the relationship between dose and the corresponding TGI (tumor growth inhibition).

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Hu-Lowe D D, Zou H Y, Grazzini M L, et al.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, 3. Clinical Cancer Research, 2008, 14(22): 7272-7283.

Background

Axitinib is a selective and oral inhibitor of vascular endothelial growth factor (VEGF) receptor tyrosine kinases 1, 2 and 3 with [1].

Axitinib inhibited the phosphorylation of VEGFR-1, 2 and 3 with IC50 values of 1.2 nM, 0.2 nM and 0.1 to 0.3 nM in cells, respectively. In HUVEC cells, Axitinib inhibited VEGFR-2 stimulated cell survival with about 1000-fold selectivity against FGFR-1. Axitinib also significantly suppressed the phosphorylation of VEGF downstream signaling molecules including Akt, eNOS and ERK1/2. Besides that, axitinib inhibited VEGFR-2 phosphorylation with EC50 value of 0.49 nM in vivo. It delayed tumore growth of human xenograft tumors in mice such as M24met, HCT-116 and SN12C [1].

References:
[1] Hu-Lowe D D, Zou H Y, Grazzini M L, et al. 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, 3. Clinical Cancer Research, 2008, 14(22): 7272-7283.

Chemical Properties

Cas No. 319460-85-0 SDF
Synonyms AG 013736
Chemical Name N-methyl-2-[[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]sulfanyl]benzamide
Canonical SMILES CNC(=O)C1=CC=CC=C1SC2=CC3=C(C=C2)C(=NN3)C=CC4=CC=CC=N4
Formula C22H18N4OS M.Wt 386.47
Solubility ≥ 19.3mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.5875 mL 12.9376 mL 25.8752 mL
5 mM 0.5175 mL 2.5875 mL 5.175 mL
10 mM 0.2588 mL 1.2938 mL 2.5875 mL
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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 2 reference(s) in Google Scholar.)

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