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Axitinib (AG 013736)VEGFR1/ c-Kit inhibitor

Axitinib (AG 013736)

Catalog No. A8370
Size Price Stock Qty
10mM (in 1mL DMSO) $55.00 In stock
50mg $50.00 In stock
100mg $85.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Chemical structure

Axitinib

Biological Activity

Description Axitinib is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 values of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM, respectively.
Targets VEGFR1/FLT1 VEGFR2/Flk1 VEGFR2/KDR VEGFR3 PDGFRβ c-Kit
IC50 0.1 nM 0.18 nM 0.2 nM 0.1 nM-0.3 nM 1.6 nM 1.7 nM

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.

Reacting condition

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

Application

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.

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Chemical Properties

Cas No. 319460-85-0 SDF Download 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 Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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.