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    Binimetinib ( Mektovi; ARRY438162; ARRY162; MEK162)
    Binimetinib ( Mektovi; ARRY438162; ARRY162; MEK162)

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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 #: V0454
    CAS #: 606143-89-9Purity ≥98%

    Description: Binimetinib (trade name: Mektovi; formerly ARRY-438162; ARRY-162; MEK-162) is a highly selective and orally bioavailable MEK1/2 (mitogen-activated protein kinase kinase) inhibitor with potential antineoplastic activity. It inhibits MEK1/2 with an IC50 of 12 nM in a cell-free assay. As of June 2018, binimetinib was approved by the US FDA for the treatment of unresectable or metastatic melanoma. 

    References: Annual Reports in Medicinal Chemistry, 2007, 42, 265–278J Clin Invest. 2013 Jun;123(6):2551-63.

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    Molecular Weight (MW)441.23
    FormulaC17H15BrF2N4O3
    CAS No.606143-89-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 88 mg/mL (199.4 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)1% CMC+0.5% Tween-80: 30 mg/mL
    Synonyms

    MEK162; ARRY 162; ARRY438162; ARRY-162, ARRY-438162; MEK 162; MEK-162; ARRY162; ARRY-162; ARRY-438162; Binimetinib; Brand name: Mektovi.

    Chemical Name: 5-((4-bromo-2-fluorophenyl)amino)-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzo[d]imidazole-6-carboxamide.

    InChi Key: ACWZRVQXLIRSDF-UHFFFAOYSA-N

    InChi Code: InChI=1S/C17H15BrF2N4O3/c1-24-8-21-16-13(24)7-10(17(26)23-27-5-4-25)15(14(16)20)22-12-3-2-9(18)6-11(12)19/h2-3,6-8,22,25H,4-5H2,1H3,(H,23,26)

    SMILES Code: O=C(C1=C(NC2=CC=C(Br)C=C2F)C(F)=C3N=CN(C)C3=C1)NOCCO 


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    In Vitro

    In vitro activity: Binimetinib (formerly known as MEK162, ARRY-162, ARRY-438162; trade name: Mektovi) is a novel potent, highly selective and oral inhibitor of MEK1/2 with IC50 of 12 nM in a cell-free assay. On 6/27/2018, the US FDA approved binimetinib for the treatment of unresectable or metastatic melanoma. MEK162 showed significant antitumor activities in cell lines and animal models. MEK162 is the first targeted therapy to show activity in patients with NRAS -mutated melanoma and might offer a new option for a cancer with few effective treatments.  


    Kinase Assay: ARRY-438162 (625 nM) inhibits in vitro osteoclast differentiation with IC50 of 39 nM. ARRY-438162 (10 μM) inhibits in vitro osteoclast resorption with IC50 of 625 nM. ARRY-438162 (2 μM) weakly affects osteoblast differentiation. ARRY-438162 is a recently disclosed potent and selective ATP non-competitive MEK1/2 inhibitor, inhibits pERK in cells with an IC50 of11 nM. MEK162 (1 μM) combined with MK-2206 (2 μM) completely reverses the resistance of RSK-expressing MCF7 cells.


    Cell Assay: MCF7 cells infected as indicated are seeded in 12-well plates (2×104). After 24 hours, cells are treated with BEZ235 (100 or 200 nM), BKM120 (0.75 or 1 μM), GDC-0941 (1 μM), or MK2206 (2 μM) alone or in combination with MEK162 (1 μM), BI-D1870 (10 μM), or AZD6244 (1 μM), as indicated in text. Cell numbers are quantified by fixing cells with 4% glutaraldehyde or methanol, washing the cells twice in H2O, and staining the cells with 0.1% crystal violet. The dye is subsequently extracted with 10% acetic acid, and its absorbance is determined (570 nm). Growth curves are performed in triplicate. Viability assays with CellTiter-Glo are performed by plating 2,000 cells in 96-well plates, adding the drug at 24 hours, and assaying 4 to 5 days after drug addition. Cell-cycle and hypodiploid apoptotic cells are quantified by flow cytometry. Briefly, cells are washed with PBS, fixed in cold 70% ethanol, and then stained with propidium iodide while being treated with RNase. Quantitative analysis of sub-G1 cells is carried out in a FACScalibur cytometer using Cell Quest software

    In VivoARRY-438162 (10 mg/kg, po, bid) reduces disease severity in a dose-related manner in rat collagen-induced arthritis (CIA) and rat adjuvant-induced arthritis (AIA) models. ARRY-438162 (po, bid) inhibits increases in ankle diameter by 27% and 50% at 1 mg/kg and 3 mg/kg in the rat collagen-induced arthritis (CIA) model, while ibuprofen has 46% inhibition. ARRY-438162 (10 mg/kg, po, bid) significantly inhibits lesions (inflammation, cartilage damage, pannus formation and bone resorption) by 32% and 60% at 1 mg/kg and 3 mg/kg in the rat collagen-induced arthritis (CIA) model. ARRY-438162 inhibits AIA ankle diameter 11% and 34% at 3 mg/kg and 10 mg/kg in rat adjuvant-induced arthritis (AIA) models. ARRY-438162 demonstrates dose-related inhibition of ankle swelling in rat adjuvant-induced arthritis (AIA) models, significant at 10 mg/kg and 30 mg/kg when compared to vehicle control. ARRY-438162 demonstrates dose-related inhibition of serum IL-6 concentration in rat adjuvant-induced arthritis (AIA) models, with complete inhibition at 10 mg/kg when compared to vehicle control. ARRY-438162 (30 mg/kg) demonstrates dose-related inhibition of relative spleen weights in rat adjuvant-induced arthritis (AIA) models. ARRY-438162 (30 mg/kg) significantly inhibits bone resorption and inflammation with delayed dosing when compared to vehicle in rat adjuvant-induced arthritis (AIA) models. MEK162 (6 mg/kg, BID) combined with BEZ235 results in a significant reduction of tumor growth in immunodeficient mice injected with MCF7 cells
    Animal modelImmunodeficient mice injected with MCF7-RSK4 cells.
    Formulation & DosageFormulated in 0.5% Tween-80, 1% carboxymethyl cellulose; 6 mg/kg; oral gavage
    ReferencesAnnual Reports in Medicinal Chemistry, 2007, 42, 265–278J Clin Invest. 2013 Jun;123(6):2551-63.


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

    Binimetinib

    Inhibition of ERK/RSK signaling overcomes resistance to PI3K inhibitors. J Clin Invest. 2013 Jun;123(6):2551-63.

    Binimetinib

    Aberrant activation of MEK signaling confers the regained growth of Her2 positive mammary tumors.  2016 Jun 9;35(23):2961-70.

    Binimetinib

    PI3K activation confers intrinsic resistance to Her2 inhibition by lapatinib.  2016 Jun 9;35(23):2961-70.


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