Binimetinib (MEK162)

For research use only.

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

53 publications

Binimetinib (MEK162) Chemical Structure

CAS No. 606143-89-9

Binimetinib (MEK162, ARRY-162, ARRY-438162) is a potent inhibitor of MEK1/2 with IC50 of 12 nM in a cell-free assay. Binimetinib induces G1 cell cycle arrest and apoptosis in human NSCLC cell lines and induces autophagy. Phase 3.

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Selleck's Binimetinib (MEK162) has been cited by 53 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. Binimetinib induces G1 cell cycle arrest and apoptosis in human NSCLC cell lines and induces autophagy. 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 M1vXVGZ2dmO2aX;uJIF{e2G7 NFT1TXlKSzVyPUGxOUBvVQ>? M{jLU|MxOzV{NU[1
Mel IL MULDfZRwfG:6aXPpeJkh[XO|YYm= M{Lh[GlEPTB;Mz63JOKyKDBwMjFOwG0> MoDwN|A2PTF3MUW=
Mel IL/R MnjER5l1d3SxeHnjbZR6KGG|c3H5 NVy3NYZUUUN3ME2yMlchyrFiMD6zJO69VQ>? MVKzNFU2OTVzNR?=
Mel Z NE[w[ZJEgXSxdH;4bYNqfHliYYPzZZk> MVTJR|UxRTNwODFCtUAxNjJizszN MnHjN|A2PTF3MUW=
A375 MYPDfZRwfG:6aXPpeJkh[XO|YYm= NYfsSXVvUUN3ME25MlghyrFiMD6xJO69VQ>? NYTzeW9mOzB3NUG1NVU>
Mel Me MoTkR5l1d3SxeHnjbZR6KGG|c3H5 NVTn[2xYUUN3ME2xN{4{KMLzIECuN{DPxE1? NGXzTG8{ODV3MUWxOS=>
Mel MTP NFXUc2xEgXSxdH;4bYNqfHliYYPzZZk> MV\JR|UxRTFyLkKgxtEhOC52IN88US=> NX3rTWNqOzB3NUG1NVU>
U2OS cells NWrP[2xZTnWwY4Tpc44h[XO|YYm= MXKxJO69VQ>? M1Py[G1GUzF4MjDicI9kc2WmIFXST{Bi[3SrdnH0bY9vKCiyLVXST|EwOiliaX6gR3o1OTVvdILlZZRm\CCXMl;TJINmdGy| NILndVYzQTF|N{K0NS=>
CHP-212 MXzD[YxtKH[rYXLpcIl1gSCjc4PhfS=> MoTXNVIxyqCq NUfqc2Y4UUN3ME2wMlAxQDNizszN Mn2xNlY6OjV6NEG=
SK-N-AS NGW5PGVE\WyuII\pZYJqdGm2eTDhd5NigQ>? Mn:xNVIxyqCq M4\EdmlEPTB;MD6wOlch|ryP NIDhWYkzPjl{NUi0NS=>
SK-N-BE(2) NXXVZmFwS2WubDD2bYFjcWyrdImgZZN{[Xl? MlyzNVIxyqCq MW\JR|UxRTBwMkig{txO M4PLT|I3QTJ3OESx
SJ-NB-10 Mlm2R4VtdCC4aXHibYxqfHliYYPzZZk> M1LxW|EzOMLiaB?= MoL6TWM2OD1zLkG2JO69VQ>? NG[3PFQzPjl{NUi0NS=>
CHP-134 MYTD[YxtKH[rYXLpcIl1gSCjc4PhfS=> M{XBNlEzOMLiaB?= NVG2ToZmUUN3ME6xOUDPxE1? M1fScVI3QTJ3OESx
Kelly NITxO4tE\WyuII\pZYJqdGm2eTDhd5NigQ>? MVSxNlDDqGh? NInpU4hKSzVyPkG1JO69VQ>? MkDqNlY6OjV6NEG=
LAN-5 M{X3OmNmdGxidnnhZoltcXS7IHHzd4F6 NGO5W|MyOjEEoHi= MnzDTWM2OD5zNTFOwG0> NXnCWXhDOjZ7MkW4OFE>
NGP MonsR4VtdCC4aXHibYxqfHliYYPzZZk> NHj2dI0yOjEEoHi= M3LBcGlEPTB-MUWg{txO MkewNlY6OjV6NEG=
SK-N-DZ MYDD[YxtKH[rYXLpcIl1gSCjc4PhfS=> NIf5dXAyOjEEoHi= M3jrdGlEPTB-MUWg{txO MoXFNlY6OjV6NEG=
A549 Mnq3R4VtdCCleXPs[UBie3OjeR?= MXKwMEAxNjVuIEGg{txO MVq0PIg> NETWcnFifCC{ZXzheIl3\Wy7IHzve{Bkd26lZX70doF1cW:wIILhcodmeyEkibSgNUDPxE1iKHWu[{4tKDBwNTDhcoQhOSEQvF2pJIlv\HWlZXSgS|Eh[XK{ZYP0 NV76WGpjOjV7M{eyPVk>
H157 MmDQR4VtdCCleXPs[UBie3OjeR?= NVP0d2RzOCxiMD61MEAyKM7:TR?= M{L6d|Q5cA>? MmC0ZZQhemWuYYTpeoVtgSCub4egZ49v[2WwdILheIlwdiC{YX7n[ZMh6onmIEGg{txOKCinLneuMEAxNjViYX7kJFEh|ryPKTDpcoR2[2WmIFexJIFzemW|dB?= NVy1XldZOjV7M{eyPVk>
H522 NYTyPWpjS2WubDDjfYNt\SCjc4PhfS=> NVHje25pOCxiMD61MEAyKM7:TR?= M{nmNFQ5cA>? M4LWRoF1KHKnbHH0bZZmdHlibH;3JINwdmOnboTyZZRqd25icnHu[4V{KOLLpDCxJO69VSBqZT7nMkwhOC53IHHu[EAyKM7:TTmgbY5lfWOnZDDHNUBienKnc4S= NIXNeoozPTl|N{K5PS=>

... 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.
  • 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 ARRY-162,ARRY-438162
Smiles CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)F)C(=O)NOCCO

In vivo Formulation Calculator (Clear solution)

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Molarity Calculator

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

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04657991 Not yet recruiting Drug: Encorafenib|Drug: Binimetinib|Drug: Pembrolizumab Melanoma Pfizer|Merck Sharp & Dohme Corp. January 29 2021 Phase 3
NCT04543188 Not yet recruiting Drug: PF-07284890|Drug: Binimetinib|Drug: Midazolam Malignant Melanoma|Carcinoma Non-Small-Cell Lung|Brain Neoplasms Primary|Brain Neoplasms|Malignant Neoplasms Pfizer September 25 2020 Phase 1
NCT03878719 Recruiting Drug: binimetinib|Drug: encorafenib Melanoma Pfizer|Pierre Fabre Laboratories August 13 2020 Phase 1
NCT04045691 Recruiting Drug: Encorafenib|Drug: Binimetinib Melanoma Stage IV|Melanoma Stage III Pierre Fabre Pharma GmbH|Pierre Fabre Pharma Austria|Pierre Fabre Pharma AG October 17 2019 --

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.

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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