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Axitinib

Cat. No. M1658
Axitinib Structure
Synonym:

AG-013736

Size Price Availability Quantity
10mM/1mL In DMSO USD 80 In stock
100mg USD 90 In stock
200mg USD 150 In stock
500mg USD 300 In stock
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Quality Control
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.

Protocol
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 nmol/l to 10 lmol/l
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 386.47
Formula C22H18N4OS
CAS Number 319460-85-0
Purity 98.86%
Solubility DMSO
Storage at -20°C
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.
Rating
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.
Rating
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).
Rating
Product Citations
References

Comprehensive overview of axitinib development in solid malignancies: focus on metastatic renal cell carcinoma.
Carmichael et al. Clin Adv Hematol Oncol. 2012 May;10(5):307-14. PMID: 22706540.

Evaluation of the effect of food on the pharmacokinetics of axitinib in healthy volunteers.
Pithavala et al. Cancer Chemother Pharmacol. 2012 Jul;70(1):103-12. PMID: 22644797.

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  Catalog
Abmole Inhibitor Catalog 2017




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

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