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.

Cited by 30 Publications

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]
(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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H727 MnvqSpVv[3Srb36gZZN{[Xl? NEezV2ZKSzVyPUGxOUBvVQ>? NFnxcnA{ODN3MkW2OS=>
Mel IL MVXDfZRwfG:6aXPpeJkh[XO|YYm= NFPWRnJKSzVyPUOuO{DDuSByLkKg{txO NHP6Um4{ODV3MUWxOS=>
Mel IL/R NUTG[m1FS3m2b4TvfIlkcXS7IHHzd4F6 M{f3NmlEPTB;Mj63JOKyKDBwMzFOwG0> MoqyN|A2PTF3MUW=
Mel Z MXPDfZRwfG:6aXPpeJkh[XO|YYm= MXHJR|UxRTNwODFCtUAxNjJizszN NYW4U21YOzB3NUG1NVU>
A375 MVnDfZRwfG:6aXPpeJkh[XO|YYm= M2rGS2lEPTB;OT64JOKyKDBwMTFOwG0> NV7wdmd1OzB3NUG1NVU>
Mel Me Mk[1R5l1d3SxeHnjbZR6KGG|c3H5 NU[wRZlRUUN3ME2xN{4{KMLzIECuN{DPxE1? M4TiU|MxPTVzNUG1
Mel MTP NWr4fmNTS3m2b4TvfIlkcXS7IHHzd4F6 M2DBOGlEPTB;MUCuNkDDuSByLkSg{txO MlKwN|A2PTF3MUW=
U2OS cells NVSwPZE4TnWwY4Tpc44h[XO|YYm= MVmxJO69VQ>? NV\jVJZmVUWNMU[yJIJtd2OtZXSgSXJMKGGldHn2ZZRqd25iKICtSXJMOS9{KTDpckBEYjRzNT30doVifGWmIGWyU3Mh[2WubIO= MljjNlkyOzd{NEG=
CHP-212 Mk\MR4VtdCC4aXHibYxqfHliYYPzZZk> NHrYNHAyOjEEoHi= M1LPUGlEPTB;MD6wNFg{KM7:TR?= MYmyOlkzPTh2MR?=
SK-N-AS NHK5dXdE\WyuII\pZYJqdGm2eTDhd5NigQ>? MmPwNVIxyqCq MWrJR|UxRTBwME[3JO69VQ>? MXKyOlkzPTh2MR?=
SK-N-BE(2) MkfNR4VtdCC4aXHibYxqfHliYYPzZZk> MX:xNlDDqGh? NU\XZodHUUN3ME2wMlI5KM7:TR?= NV;nRYRWOjZ7MkW4OFE>
SJ-NB-10 MmOyR4VtdCC4aXHibYxqfHliYYPzZZk> M4XNV|EzOMLiaB?= MorCTWM2OD1zLkG2JO69VQ>? MnuxNlY6OjV6NEG=
CHP-134 NIfJboNE\WyuII\pZYJqdGm2eTDhd5NigQ>? MX[xNlDDqGh? NFuwZ4pKSzVyPkG1JO69VQ>? NFfpZW8zPjl{NUi0NS=>
Kelly MYPD[YxtKH[rYXLpcIl1gSCjc4PhfS=> NIfEeoMyOjEEoHi= MoTDTWM2OD5zNTFOwG0> NV36WVhmOjZ7MkW4OFE>
LAN-5 MV7D[YxtKH[rYXLpcIl1gSCjc4PhfS=> M1HiWFEzOMLiaB?= M4X2U2lEPTB-MUWg{txO MnfONlY6OjV6NEG=
NGP MmP4R4VtdCC4aXHibYxqfHliYYPzZZk> MUKxNlDDqGh? MVrJR|UxRjF3IN88US=> M1nvW|I3QTJ3OESx
SK-N-DZ NXz2d5p2S2WubDD2bYFjcWyrdImgZZN{[Xl? MnvjNVIxyqCq MoLLTWM2OD5zNTFOwG0> MUeyOlkzPTh2MR?=
A549 MWjD[YxtKGO7Y3zlJIF{e2G7 MYmwMEAxNjVuIEGg{txO MlnPOFhp NGLub2lifCC{ZXzheIl3\Wy7IHzve{Bkd26lZX70doF1cW:wIILhcodmeyEkibSgNUDPxE1iKHWu[{4tKDBwNTDhcoQhOSEQvF2pJIlv\HWlZXSgS|Eh[XK{ZYP0 MXmyOVk{PzJ7OR?=
H157 NFjjcZZE\WyuIHP5Z4xmKGG|c3H5 NETkOFIxNCByLkWsJFEh|ryP NVX5VIhRPDiq NUDtNWFb[XRicnXsZZRqfmWueTDsc5ch[2:wY3XueJJifGmxbjDyZY5o\XNi4pokJFEh|ryPIDjlMocvNCByLkWgZY5lKDFizszNLUBqdmS3Y3XkJGcyKGG{cnXzeC=> NWPXXmtUOjV7M{eyPVk>
H522 NY[0fWViS2WubDDjfYNt\SCjc4PhfS=> NIqyS4YxNCByLkWsJFEh|ryP NFPXWJI1QGh? M4jwPIF1KHKnbHH0bZZmdHlibH;3JINwdmOnboTyZZRqd25icnHu[4V{KOLLpDCxJO69VSBqZT7nMkwhOC53IHHu[EAyKM7:TTmgbY5lfWOnZDDHNUBienKnc4S= M3j5TVI2QTN5Mkm5

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
MEK / p-MEK / ERK / p-ERK ; 

PubMed: 26925841     


Binimetinib inhibits RAS/MAPK pathway activity. Neuroblastoma cells were treated with 1 μM binimetinib for 1 h and then lysed and Western blots for total MEK, phospho-MEK (p-MEK), total ERK, and phospho-ERK (p-ERK) were performed. Actin was used as a loading control.

p-KIT / KIT / ETV1 ; 

PubMed: 25572173     


Immunoblot of ETV1, pKIT and pERK levels in GIST882 and GIST-T1 cells treated with Imatinib (500 nM) or MEK162 (1 μM) for the indicated time points.

26925841 25572173
Growth inhibition assay
Cell viability; 

PubMed: 26925841     


e CHP-134, Kelly, LAN-5, NGP, and SK-N-DZ cells maintain resistance to binimetinib treatment after 120 h of drug exposure. f IC50 values (μM) were calculated for cells treated with binimetinib for 120 h.

26925841
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]
- Collapse
  • 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 to the product individually and in order(Data is from Selleck tests instead of citations):
1% CMC+0.5% Tween-80
For best results, use promptly after mixing.
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
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 (mg) = Concentration (mM) × Volume (mL) × 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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03878719 Recruiting Drug: binimetinib|Drug: encorafenib Melanoma Array BioPharma|Pierre Fabre Laboratories December 2019 Phase 1
NCT04005144 Not yet recruiting Drug: Binimetinib|Drug: Brigatinib ALK Gene Rearrangement|Lung Non-Small Cell Carcinoma|Progressive Disease|ROS1 Gene Rearrangement|Stage IIIB Lung Cancer|Stage IIIC Lung Cancer|Stage IV Lung Cancer|Stage IVA Lung Cancer|Stage IVB Lung Cancer University of California San Francisco|Takeda|Array BioPharma November 1 2019 Phase 1
NCT04109456 Not yet recruiting Drug: IN10018|Drug: Binimetinib Metastatic Melanoma InxMed (Shanghai) Co. Ltd. November 30 2019 Phase 1
NCT04045691 Not yet recruiting Drug: Encorafenib|Drug: Binimetinib Melanoma Stage IV|Melanoma Stage III Pierre Fabre Pharma GmbH|Pierre Fabre Pharma Austria August 2019 --
NCT03911869 Recruiting Drug: encorafenib|Drug: binimetinib Brain Metastases Array BioPharma June 13 2019 Phase 2
NCT03839342 Recruiting Drug: Binimetinib|Drug: Encorafenib Solid Tumor University Health Network Toronto June 7 2019 Phase 2

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

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

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