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Axitinib

Cat. No. M1658

All AbMole products are for research use only, cannot be used for human consumption.

Axitinib Structure
Synonym:

AG-013736

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 50  USD50 In stock
50mg USD 45  USD45 In stock
100mg USD 70  USD70 In stock
200mg USD 90  USD90 In stock
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Quality Control & Documentation
Biological Activity

Axitinib blocked phosphorylation of VEGFR-2 and VEGFR-3 with average IC50s of 0.2 and 0.1 to 0.3 nM.Axitinib (also known as AG013736) is a small molecule tyrosine kinase inhibitor.It inhibits multiple targets, including VEGFR-1, VEGFR-2, VEGFR-3, platelet derived growth factor receptor (PDGFR), and cKIT (CD117). It has been shown to significantly inhibit growth of breast cancer in xenograft models and has been successful in trials with renal cell carcinoma (RCC) and several other tumor types.

Product Citations
Customer Product Validations & Biological Datas
Source Int J Cancer (2017) . Figure 6. Axitinib (20 mg/kg, Abmole Bioscience)
Method
Cell Lines Hmga2/T mice
Concentrations 20mg/kg
Incubation Time 6 weeks
Results Together, these results show that, while bromocriptine and/or axitinib were able to correct structuralabnormalities of tumoral vessels with a similar efficacy, only the combination treatment restored their function.
Source Int J Cancer (2017) . Figure 5. Axitinib (20 mg/kg, Abmole Bioscience)
Method
Cell Lines Hmga2/T mice
Concentrations 20mg/kg
Incubation Time 6 weeks
Results Analysis of pituitary vasculature in various conditions and morphometric measurements of blood vessels demonstrate that D2R agonist or axitinib had an equivalent capacity to improve structural defects present in tumoral blood vessels and that the combination treatment did not lead to a significant advantage.
Source Int J Cancer (2017) . Figure 4. Axitinib (20 mg/kg, Abmole Bioscience)
Method
Cell Lines Hmga2/T mice
Concentrations 20mg/kg
Incubation Time 6 weeks
Results Importantly, the expression of Angpt1 and Prok1, which was upregulated in response to bromocriptine treatment, was unchanged and remained low after axitinib treatment (Fig. 4d).
Protocol (for reference only)
Cell Experiment
Cell lines HUVEC, SH-SY5Y, IGR-N91 and IGR-NB8 cell lines
Preparation method MTS cell proliferation assay
HUVEC, SH-SY5Y, IGR-N91 and IGR-NB8 cell lines were seeded at 5,000 cells per well in a 96-well plate and left to settle overnight in EMBV R-2 or DMEM with 10% fetal calf serum. The cells were treated with axitinib at concentrations ranging from 1 nmol/l to 10 lmol/l. Cell viability was determined after 72 hr using MTS tetrazolium substrate (CellTiter 96 Aqueous One Solution Cell Proliferation Assay; Promega Corporation, Charbonnieres, France) and colorimetric measurement at 490 nm in an automatic plate reader (Elx808; Fisher Bioblock Scientific SAS, Illkirch, France). IC50 values were calculated using GraphPadV R Prism software (version 3.00).
Concentrations 1 nM - 10 μM
Incubation time 72 hr
Animal Experiment
Animal models IGR-N91 xenografts with female SPF-Swiss athymic nude mice at 6–8 weeks of age
Formulation 0.5% CMC
Dosages 30 mg/kg BID for 2 weeks
Administration oral gavage
Chemical Information
Molecular Weight 386.47
Formula C22H18N4OS
CAS Number 319460-85-0
Solubility (25°C) DMSO ≥ 20 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Carmichael et al. Clin Adv Hematol Oncol. Comprehensive overview of axitinib development in solid malignancies: focus on metastatic renal cell carcinoma.

[2] Pithavala et al. Cancer Chemother Pharmacol. Evaluation of the effect of food on the pharmacokinetics of axitinib in healthy volunteers.

[3] Jochen Rössler, et al. Int J Cancer. The selective VEGFR1-3 inhibitor axitinib (AG-013736) shows antitumor activity in human neuroblastoma xenografts

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  Catalog
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Keywords: Axitinib, AG-013736 supplier, VEGFR/PDGFR, inhibitors, activators

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