Binimetinib (MEK162)

For research use only.

Catalog No.S7007 Synonyms: ARRY-162,ARRY-438162

44 publications

Binimetinib (MEK162) 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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Selleck's Binimetinib (MEK162) has been cited by 44 publications

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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.
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
Mel IL MnnNR5l1d3SxeHnjbZR6KGG|c3H5 Ml7YTWM2OD1|LkegxtEhOC5{IN88US=> NXH3OoJCOzB3NUG1NVU>
Mel IL/R MmjHR5l1d3SxeHnjbZR6KGG|c3H5 MmP2TWM2OD1{LkegxtEhOC5|IN88US=> MUWzNFU2OTVzNR?=
Mel Z NVS5flV5S3m2b4TvfIlkcXS7IHHzd4F6 NXWwdGlmUUN3ME2zMlghyrFiMD6yJO69VQ>? NHTMfXU{ODV3MUWxOS=>
Mel Me M33rdGN6fG:2b4jpZ4l1gSCjc4PhfS=> NHrDRYRKSzVyPUGzMlMhyrFiMD6zJO69VQ>? Mli2N|A2PTF3MUW=
U2OS cells MVzGeY5kfGmxbjDhd5NigQ>? NYr5bFJOOSEQvF2= MUDNSWsyPjJiYnzvZ4tm\CCHUlugZYN1cX[jdHnvckApeC2HUluxM|IqKGmwIFPaOFE2NXS{ZXH0[YQhXTKRUzDj[Yxtew>? MX:yPVE{PzJ2MR?=
CHP-212 NEHMRlBE\WyuII\pZYJqdGm2eTDhd5NigQ>? NF\JbmIyOjEEoHi= MnnPTWM2OD1yLkCwPFMh|ryP MXuyOlkzPTh2MR?=
SK-N-AS NXjTUo9LS2WubDD2bYFjcWyrdImgZZN{[Xl? NH\sepQyOjEEoHi= NVHKNVk6UUN3ME2wMlA3PyEQvF2= NHnjeGszPjl{NUi0NS=>
SK-N-BE(2) Mn\VR4VtdCC4aXHibYxqfHliYYPzZZk> NEjP[mUyOjEEoHi= MmHSTWM2OD1yLkK4JO69VQ>? MXWyOlkzPTh2MR?=
CHP-134 MlrJR4VtdCC4aXHibYxqfHliYYPzZZk> MnzyNVIxyqCq NVXTfnlnUUN3ME6xOUDPxE1? M1K5fVI3QTJ3OESx
Kelly MoXVR4VtdCC4aXHibYxqfHliYYPzZZk> NHzVUo8yOjEEoHi= M17CVGlEPTB-MUWg{txO NX71T4V[OjZ7MkW4OFE>
NGP M3i1cWNmdGxidnnhZoltcXS7IHHzd4F6 NUn6eGpbOTJywrDo NEHwc3pKSzVyPkG1JO69VQ>? MVuyOlkzPTh2MR?=
A549 NFXUdGRE\WyuIHP5Z4xmKGG|c3H5 MmXHNEwhOC53LDCxJO69VQ>? NEjBTnk1QGh? Mn35ZZQhemWuYYTpeoVtgSCub4egZ49v[2WwdILheIlwdiC{YX7n[ZMh6onmIEGg{txOKCinLneuMEAxNjViYX7kJFEh|ryPKTDpcoR2[2WmIFexJIFzemW|dB?= NIT5enAzPTl|N{K5PS=>
H157 NXzGZZF3S2WubDDjfYNt\SCjc4PhfS=> Mm\sNEwhOC53LDCxJO69VQ>? MY[0PIg> NGexOYRifCC{ZXzheIl3\Wy7IHzve{Bkd26lZX70doF1cW:wIILhcodmeyEkibSgNUDPxE1iKHWu[{4tKDBwNTDhcoQhOSEQvF2pJIlv\HWlZXSgS|Eh[XK{ZYP0 NWjScpVUOjV7M{eyPVk>
H522 NXnQcpJxS2WubDDjfYNt\SCjc4PhfS=> MlPKNEwhOC53LDCxJO69VQ>? NXu0UoZkPDiq M3vCSoF1KHKnbHH0bZZmdHlibH;3JINwdmOnboTyZZRqd25icnHu[4V{KOLLpDCxJO69VSBqZT7nMkwhOC53IHHu[EAyKM7:TTmgbY5lfWOnZDDHNUBienKnc4S= M3HqT|I2QTN5Mkm5

... Click to View More Cell Line Experimental Data

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.

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]


Animal Research:[4]
- Collapse
  • Animal Models: immunodeficient mice injected with MCF7-RSK4 cells.
  • 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


CAS No. 606143-89-9
Storage powder
in solvent
Synonyms ARRY-162,ARRY-438162
Smiles C[N]1C=NC2=C1C=C(C(=O)NOCCO)C(=C2F)NC3=C(F)C=C(Br)C=C3

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03878719 Recruiting Drug: binimetinib|Drug: encorafenib Melanoma Pfizer|Pierre Fabre Laboratories June 12 2020 Phase 1
NCT04005144 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 December 6 2019 Phase 1
NCT04045691 Recruiting Drug: Encorafenib|Drug: Binimetinib Melanoma Stage IV|Melanoma Stage III Pierre Fabre Pharma GmbH|Pierre Fabre Pharma Austria October 17 2019 --
NCT03911869 Recruiting Drug: encorafenib|Drug: binimetinib Brain Metastases Array BioPharma June 13 2019 Phase 2
NCT03839342 Active not recruiting Drug: Binimetinib|Drug: Encorafenib Solid Tumor University Health Network Toronto June 7 2019 Phase 2

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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.

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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