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.

Size Price Stock Quantity  
USD 97 In stock
USD 370 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

3 Customer Reviews

  • 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.

  • 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.

Purity & Quality Control

Choose Selective MEK Inhibitors

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]
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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 1% CMC+0.5% Tween-80 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

MEK Signaling Pathway Map

Related MEK Products

Tags: buy Binimetinib (MEK162, ARRY-162, ARRY-438162) | Binimetinib (MEK162, ARRY-162, ARRY-438162) supplier | purchase Binimetinib (MEK162, ARRY-162, ARRY-438162) | Binimetinib (MEK162, ARRY-162, ARRY-438162) cost | Binimetinib (MEK162, ARRY-162, ARRY-438162) manufacturer | order Binimetinib (MEK162, ARRY-162, ARRY-438162) | Binimetinib (MEK162, ARRY-162, ARRY-438162) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID