Binimetinib (MEK162, ARRY-162, ARRY-438162)

Catalog No.S7007

Binimetinib (MEK162, ARRY-162, ARRY-438162) Chemical Structure

Molecular Weight(MW): 441.23

Binimetinib (MEK162, ARRY-162, ARRY-438162) is a potent inhibitor of MEK1/2 with IC50 of 12 nM in a cell-free assay. Phase 3.

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5 Customer Reviews

  • Cells seeded in 96-well plates (2,000-3,000 cells per well) were cultured in triplicate with or without graded concentrations of MEK1/2 plus/minus 100 μg/mL cetuximab, which were not renewed during the entire period of cell exposure. For each pair of columns, the height of the left columns represents the sum of the toxic effect of each agent and, therefore, the expected toxicity if their effects were additive when used in combination. The total height of the right columns represents the observed toxicity when the agents were used in combination. The difference between the heights of the paired columns reflects the magnitude of antagonism or synergism on cell toxicity between MEK1/2 inhibitors and cetuximab in NRAS+/+ (left panels) and NRASQ61K/+ (right panels) cells. Results are shown as mean (columns) ± SD (error bars) from at least three experiments in which triplicate wells were analyzed.

    Oncotarget, 2016, 7(50):82185-82199. Binimetinib (MEK162, ARRY-162, ARRY-438162) purchased from Selleck.

    H460 cells were either treated with perifosine (3 μM), MEK-162 (1 μM), or combine for 8 h; expression of indicated proteins was tested by Western blots using corresponding antibodies.

    Tumor Biol, 2015, 36: 5699-06. Binimetinib (MEK162, ARRY-162, ARRY-438162) purchased from Selleck.

  • H460 cells were treated with indicated concentration of perifosine (1–3 μM), in the presence or absence of MEK-162 (1 μM) for 48 h, cell apoptosis was tested by either Annexin V FACS assay or histone-DNA apoptosis ELISA assay.

    Tumor Biol, 2015, 36: 5699-06. Binimetinib (MEK162, ARRY-162, ARRY-438162) purchased from Selleck.

    B: ERK and p-ERK1/2 levels in response to MEKi treatment. Tra = trametinib, Ref = refametinib, Sel = selumetinib, Bin = binimetinib. Films were intentionally overexposed to detect signal in lanes with low p-ERK1/2 expression. For each cell line all treatment conditions were performed as part of the same experiment. All experimental findings were confirmed in independent experiments performed in triplicate. Note: membranes incubated with p-ERK1/2 antibody were overexposed to capture all remaining signal after MEKi treatment. WB images have been cut to keep the same sample order. All membranes incubated with the same antibody have been exposed for the same period of time.

    Am J Cancer Res, 2016, 6(10):2235-2251. Binimetinib (MEK162, ARRY-162, ARRY-438162) purchased from Selleck.

  • HepG2 cells, “Pnt-2” primary HCC cells or THLE-2 normal liver cells were pretreated with PD-98059 (1 mM) or MEK-162 (“MEK”, 1 mM) for 1 h prior toWAY-600 (“WAY”, 100 nM) treatment, after applied period, cell viability and apoptosis were tested by MTT assay (F and H).

    Biochem Biophys Res Commun, 2016, 474(2):330-7.. Binimetinib (MEK162, ARRY-162, ARRY-438162) purchased from Selleck.

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Biological Activity

Description Binimetinib (MEK162, ARRY-162, ARRY-438162) is a potent inhibitor of MEK1/2 with IC50 of 12 nM in a cell-free assay. Phase 3.
Targets
MEK [1]
(Cell-free assay)
12 nM
In vitro

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. [2] ARRY-438162 is a recently disclosed potent and selective ATP non-competitive MEK1/2 inhibitor, inhibits pERK in cells with an IC50 of11 nM. [3] MEK162 (1 μM) combined with MK-2206 (2 μM) completely reverses the resistance of RSK-expressing MCF7 cells. [4]

In vivo ARRY-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. [1] 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. [2] MEK162 (6 mg/kg, BID) combined with BEZ235 results in a significant reduction of tumor growth in immunodeficient mice injected with MCF7 cells. [4]

Protocol

Animal Research:[4]
+ Expand
  • Animal Models: immunodeficient mice injected with MCF7-RSK4 cells.
  • Formulation: 0.5% Tween-80, 1% carboxymethyl cellulose
  • Dosages: 6 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 88 mg/mL warmed (199.44 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
1% CMC+0.5% Tween-80
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 441.23
Formula

C17H15BrF2N4O3

CAS No. 606143-89-9
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02185690 Not yet recruiting Lungcancer University Health Network, Toronto|Novartis Pharmaceuticals March 2017 Phase 1
NCT02964689 Not yet recruiting Advanced Non-small Cell Lung Cancer|KRAS Gene Mutation|Lung Cancer Swiss Group for Clinical Cancer Research March 2017 Phase 1
NCT02902042 Not yet recruiting Malignant Melanoma Prof. Dr. med. Dirk Schadendorf|University Hospital, Essen December 2016 Phase 1|Phase 2
NCT02631447 Recruiting Metastatic Melanoma Fondazione Melanoma Onlus|Clinical Research Technology S.r.l. November 2016 Phase 2
NCT02928224 Recruiting BRAF V600E-mutant Metastatic Colorectal Cancer Array BioPharma|Merck KGaA|Pierre Fabre Medicament August 2016 Phase 3
NCT02451865 Withdrawn Recurrent Non-Small Cell Lung Carcinoma|Stage IV Non-Small Cell Lung Cancer Jonsson Comprehensive Cancer Center|National Cancer Institute (NCI) June 2016 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    Could please clarify the formulation in vivo for S7007 is clear or not?

  • Answer:

    S7007 can be dissolved in 5% DMSO+45% PEG 300+ddH2O at 5 mg/ml clearly for injection.

MEK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID