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    Axitinib (AG-013736; Inlyta)
    Axitinib (AG-013736; Inlyta)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0492
    CAS #: 319460-85-0Purity ≥98%

    Description: Axitinib (formerly AG013736; brand name Inlyta), is a potent, orally bioavailable, small molecule and multi-targeted kinase inhibitor with potential antitumor activity. It inhibits multiple kinases such as 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 in Porcine aorta endothelial cells, respectively. Axitinib inhibits the proangiogenic cytokines VEGF and PDGF, thereby exerting an anti-angiogenic effect. It was approved by FDA for the treatment for renal cell carcinoma on 27 January 2012. 

    References: Int J Cancer. 2011 Jun 1;128(11):2748-58; Magn Reson Imaging. 2007 Apr;25(3):319-27.  

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    Molecular Weight (MW)386.47
    FormulaC22H18N4OS
    CAS No.319460-85-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 35 mg/mL (90.5 mM)
    Water: <1 mg/mL
    Ethanol:<1 mg/mL
    Solubility (In vivo)0.5% CMC: 30 mg/mL
    Synonyms

    Synonym: AG 013736; AG013736; Axitinib; AG 013736; Brand name: Inlyta.

    Chemical Name: (E)-N-methyl-2-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)benzamide

    InChi Key: RITAVMQDGBJQJZ-FMIVXFBMSA-N

    InChi Code: InChI=1S/C22H18N4OS/c1-23-22(27)18-7-2-3-8-21(18)28-16-10-11-17-19(25-26-20(17)14-16)12-9-15-6-4-5-13-24-15/h2-14H,1H3,(H,23,27)(H,25,26)/b12-9+

    SMILES Code: O=C(NC)C1=CC=CC=C1SC2=CC3=C(C=C2)C(/C=C/C4=NC=CC=C4)=NN3


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    In Vitro

    In vitro activity: Axitinib could block the cellular autophosphorylation of VEGFR and VEGF-mediated endothelial cell viability, tube formation, and downstream signaling. Axitinib inhibits the proliferation of variable cell lines with IC50 of >10,000 nM (IGR-N91), 849 nM (IGR-NB8), 274 nM (SH-SY5Y) and 573 nM (non-VEGF stimulated HUVEC).


    Kinase Assay: Porcine aorta endothelial (PAE) cells, which overexpress full-length VEGFR2, PDGFRβ, Kit, and NIH-3T3, which overexpress murine VEGFR2 (Flk-1) or PDGFRα, are generated. The 96-well plates are coated with 100 μL/well of 2.5 μg/mL anti-VEGFR2 antibody, 0.75 μg/mL anti-PDGFRβ antibody, 0.25 μg/mL anti-PDGFRα antibody, 0.5 μg/mL anti-KIT antibody, or 1.20 μg/mL anti-Flk-1 antibody to prepare ELISA capture plates. Then phosphorylation of RTK is measured by ELISA.


    Cell Assay: Cells (HUVEC, SH-SY5Y, IGR-N91 and IGR-NB8 cells) are seeded in a 96-well plate at a density of 5 × 104 and cultured for 24 hours. Axitinib is added to the cells at concentrations ranging from 1 nM to 10 μM. Cell viability is measured after 72 hours by MTS tetrazolium substrate and IC50 values are calculated.

    In VivoAxitinib exhibits primary inhibition to orthotopically transplanted models such as M24met (melanoma), HCT-116 (colorectal cancer), and SN12C (renal cell carcinoma). Axitinib delays the tumor growth with 11.4 days compared to the controls (p.o. 30 mg/kg) and decreases the Mean Vessels Density (MVD) to 21, compared to 49 in controls, in IGR-N91 flank xenografts. Axitinib significantly inhibits growth and disrupts tumor microvasculature in BT474 breast cancer model at 10-100 mg/kg. Axitinib has shown single-agent activity in variable tumors, including renal cell carcinoma, thyroid cancer, non-small cell lung cancer, and melanoma.
    Animal modelBT474 breast cancer cells are implanted subcutaneously into Immune-deficient female mice (Nu/nu; age 8-12 weeks).
    Formulation & DosageDissolved in  0.5% carboxymethylcellulose (CMC); 10, 30 or 100 mg/kg;  Oral gavage
    References

    Int J Cancer. 2011 Jun 1;128(11):2748-58; Magn Reson Imaging. 2007 Apr;25(3):319-27.  


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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