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    Selumetinib sulfate (AZD6244 sulfate)
    Selumetinib sulfate (AZD6244 sulfate)

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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 #: V37565
    CAS #: 943332-08-9Purity ≥98%

    Description: Selumetinib sulfate (also known as AZD6244 sulfate; ARRY-142886 sulfate) is a novel, potent, highly selective, orally bioavailable, and non-ATP-competitive small molecule MEK1 inhibitor with IC50 of 14 nM in cell-free assays and with anticancer activity, it also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Selumetinib inhibits mitogen-activated protein kinase kinases 1 and 2, which may prevent the activation of MEK1/2-dependent effector proteins and transcription factors, and so may inhibit cellular proliferation in MEK-overexpressing tumor cells. 

    References: Mol Cancer Ther. 2007 Jan;6(1):138-46; Clin Cancer Res. 2007 Mar 1;13(5):1576-83.


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    Molecular Weight (MW)555.76
    FormulaC₁₇H₁₇BrClFN₄O₇S
    CAS No.943332-08-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: >100 mg/mL
    Water: N/A
    Ethanol: N/A
    Solubility (In vivo)4% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5 mg/mL
    SynonymsARRY-142886 sulfate; AZD6244 sulfate; AZD-6244; AZD 6244; ARRY142886; ARRY 142886; ARRY-142886; ARRY886; ARRY-886; ARRY 886 sulfate


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    In Vitro

    In vitro activity: AZD6244 is not competitive with ATP and inactivates the ERK1/2 phosphorylation with IC50 concentrations below 40 nM. AZD6244 also inhibits the growth of primary HCC cells through inhibition of ERK1/2 and p90RSK phosphorylation, accompanied with elevation of the cleavage of caspase-3 and caspase-7, and cleaved poly(ADP)ribose polymerase. AZD6244 has little effects on the p38, c-Jun-NH2-kinase, phosphatidylinositol 3-kinase, and MEK5/ERK5 pathways. AZD6244 is sensitive to Raf mutations in breast cancer cell lines and Ras mutations in NSCLC cell lines.


    Kinase Assay: Anti-MEK1 antibody is used to immunoprecipitate MEK1 molecules. MEK kinase activity is measured as the ability of immuno-isolated MEK1 to activate recombinant ERK1 in a coupled assay using MBP as the end point of the assay. Phosphorylated MBP is resolved on a 14% SDS-PAGE gel and vacuum-dried before exposure to X-ray film.


    Cell Assay: Cells (Primary HCC cell lines including 2-1318, 4-1318 and 26-1004 cells) are seeded at a density of 2.0 × 104. After 48 hours incubation, the cells are rinsed twice with culture media. Cells are treated with various concentrations of AZD6244 for 24 or 48 hours. Cell viability is determined by the 3-(4,5-dimethylthiazol-2y1)-2,5-diphenyltetrazolium bromide (MTT) assay. Cell proliferation is assayed using a bromodeoxyuridine kit.

    In VivoAZD6244 significantly inhibits phosphorylation of ERK1/2 in 2-1318, 5-1318, 26-1004 and 4-1318 xenografts and induces apoptosis in primary 2-1318 cells by activating the caspase pathway. AZD6244 could inhibit the tumor growth in HT-29 xenograft, which is a colorectal tumor model carrying a B-Raf mutation, at a dose of 100 mg/kg and the tumor growth inhibition of AZD6244 is better than it of Gemcitabine. Otherwise AZD6244 could inhibit HCC xenografts tumor growth, which associated with increased apoptosis and down-regulation of cell cycle regulators, including cyclin D1, Cdc-2, CDK2 and 4, cyclin B1, and c-Myc
    Animal modelHCC xenografts in mice homozygous for the SCID (severe combined immunodeficiency) mutation
    Formulation & DosageDissolved in water; 50 or 100mg/kg;  Oral gavage
    References

    Mol Cancer Ther. 2007 Jan;6(1):138-46; Clin Cancer Res. 2007 Mar 1;13(5):1576-83.


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

    Selumetinib (AZD6244)

    Structure of ARRY-142886 and its ability to inhibit enzymatic MEK1 activity.  2007 Mar 1;13(5):1576-83.

    Selumetinib (AZD6244)

    Inhibition of tumor growth and decreased tumor phospho-ERK1/2 levels in a mouse HT-29 xenograft model.


    Selumetinib (AZD6244)

    Inhibition of basal and induced ERK1/2 phosphorylation in human cancer cell lines and PBMCs.  2007 Mar 1;13(5):1576-83.

    Selumetinib (AZD6244)

    Tumor growth inhibition in the mouse BxPC3 xenograft model.  2007 Mar 1;13(5):1576-83.

    Selumetinib (AZD6244)
    Selumetinib (AZD6244)


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