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    AZD8330 (ARRY704; ARRY424704)
    AZD8330 (ARRY704; ARRY424704)

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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 #: V0458
    CAS #: 869357-68-6Purity ≥98%

    Description: AZD8330 (AZD-8330; ARRY-704; ARRY-424704) is an orally bioactive and non-ATP competitive (Allosteric) MEK 1/2 inhibitor with potential anticancer activity. It inhibits MEK1/2 with an IC50 of 7 nM.

    References: Clin Cancer Res. 2007 Mar 1;13(5):1576-83; Eur J Cancer. 2013 May;49(7):1521-9.Genes Cancer. 2015 Nov;6(11-12):503-12.

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    Molecular Weight (MW)461.23
    FormulaC16H17FIN3O4
    CAS No.869357-68-6
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 92 mg/mL (199.5 mM)
    Water: <1 mg/mL
    Ethanol: 92 mg/mL (199.5 mM)
    Solubility (In vivo)0.5% hydroxyethyl cellulose+0.1% Tween 80: 30mg/mL
    Synonyms

    ARRY704; AZD 8330; AZD8330; ARRY 424704; ARRY-424704; AZD-8330; ARRY424704; ARRY-704; ARRY 704.

    Chemical Name: 2-((2-fluoro-4-iodophenyl)amino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxamide.

    InChi Key: RWEVIPRMPFNTLO-UHFFFAOYSA-N

    InChi Code: InChI=1S/C16H17FIN3O4/c1-9-7-11(15(23)20-25-6-5-22)14(21(2)16(9)24)19-13-4-3-10(18)8-12(13)17/h3-4,7-8,19,22H,5-6H2,1-2H3,(H,20,23)

    SMILES Code: O=C(C(C=C1C)=C(NC2=CC=C(I)C=C2F)N(C)C1=O)NOCCO 


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    In Vitro

    In vitro activity: AZD8330 potently and strongly inhibits MEK 1/2. AZD8330 has no inhibitory activity against over 200 other kinases including at concentrations up to 10 μM. AZD8330 demonstrates sub-nanomolar potency in mechanistic (pERK) and low to sub-nanomolar potency in functional (proliferation) assays in MEK 1/2 inhibitor sensitive cell lines.


    Kinase Assay: NH2-terminal hexahistidine tagged, constitutively active MEK1 (S218D, S222D ΔR4F) is expressed in baculovirus-infected Hi5 insect cells and purified by immobilized metal affinity chromatography, ion exchange, and gel filtration. The activity of MEK1 is assessed by measuring the incorporation of [γ- 33P]phosphate from [γ-33P]ATP onto ERK2. The assay is carried out in a 96-well polypropylene plate with an incubation mixture (100 μL) composed of 25 mM HEPES (pH 7.4), 10 mM MgCl2, 5 mM β-glycerolphosphate, 100 μM sodium orthovanadate, 5 mM DTT, 5 nM MEK1, 1 μM ERK2, and 0 to 80 nM AZD8330 (final concentration of 1% DMSO). The reactions are initiated by the addition of 10 μM ATP (with 0.5 μC k[γ-33P]ATP/well) and incubated at room temperature for 45 min. An equal volume of 25% trichloracetic acid is added to stop the reaction and precipitate the proteins. Precipitated proteins are trapped onto glass fiber B filter plates, excess labeled ATP is washed off with 0.5% phosphoric acid, and radioactivity is counted in a liquid scintillation counter. ATP dependence is determined by varying the amount of ATP in the reaction mixture. The data are globally fitted.


    Cell Assay: Malme-3M melanoma cells are plated in 96-wells and treated with various concentrations of AZD8330 for 1 hour at 37 °C. The cells are fixed, permeabilized, and incubated with an anti-phospho-ERK antibody and an anti-ERK 1/2 antibody. Plates are washed and fluorescently-labeled secondary antibodies are added. Plates are analyzed on a LICOR fluorescence imager. The pERK signal is normalized to the total ERK signal.

    In Vivo In a Calu-6 rat xenograft pharmacokinetic/pharmacodynamic (PK/PD) model a single, 1.25 mg/kg oral dose of AZD8330 inhibits ERK phosphorylation by > 90% for between 4 and 8 hours. Doses as low as 0.4 mg/kg once daily are sufficient for > 80% tumor growth inhibition in the Calu-6 nude rat xenograft model. In the Calu-6 model, AZD8330 inhibits tumor growth in a dose-dependent fashion, at 0.3 mg/kg and 1.0 mg/kg once daily
    Animal modelFemale nude rats with Calu-6 cells, nude rats with SW620 cells
    Formulation & DosageDissolved in 0.5% HPMC-0.1% Tween; 0.3, 1 mg/kg; Oral gavage
    References

    Clin Cancer Res. 2007 Mar 1;13(5):1576-83.


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

    AZD8330

    Selection of hits in two human osteosarcoma cell lines.  2015 Nov;6(11-12):503-12.

    AZD8330

    Validation of three MEK inhibitors in 6 osteosarcoma cell lines.  2015 Nov;6(11-12):503-12.

    AZD8330

    Validation of sensitivity to MEK inhibitors in a 3D culture system.  2015 Nov;6(11-12):503-12.


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