Binimetinib (MEK162)

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

For research use only.

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.

Binimetinib (MEK162) Chemical Structure

CAS No. 606143-89-9

Selleck's Binimetinib (MEK162) has been cited by 69 publications

Purity & Quality Control

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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 M{\NcmZ2dmO2aX;uJIF{e2G7 M4DBNWlEPTB;MUG1JI5O NYThb3FsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOVI2PjVpPkOwN|UzPTZ3PD;hQi=>
Mel IL MUHDfZRwfG:6aXPpeJkh[XO|YYm= MXXJR|UxRTNwNzFCtUAxNjJizszN M372dlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNUWxOVE2Lz5|MEW1NVUyPTxxYU6=
Mel IL/R NFXG[odEgXSxdH;4bYNqfHliYYPzZZk> MmPLTWM2OD1{LkegxtEhOC5|IN88US=> NGXQfIY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEW1NVUyPSd-M{C1OVE2OTV:L3G+
Mel Z MXHDfZRwfG:6aXPpeJkh[XO|YYm= NY[2SWJsUUN3ME2zMlghyrFiMD6yJO69VQ>? Mn73QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB3NUG1NVUoRjNyNUWxOVE2RC:jPh?=
A375 NXrsTIhQS3m2b4TvfIlkcXS7IHHzd4F6 M1;NZ2lEPTB;OT64JOKyKDBwMTFOwG0> NVjob4p7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C1OVE2OTVpPkOwOVUyPTF3PD;hQi=>
Mel Me NHvWelhEgXSxdH;4bYNqfHliYYPzZZk> MUXJR|UxRTF|LkOgxtEhOC5|IN88US=> NFLYRo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEW1NVUyPSd-M{C1OVE2OTV:L3G+
Mel MTP MkD1R5l1d3SxeHnjbZR6KGG|c3H5 NF;LXYpKSzVyPUGwMlIhyrFiMD60JO69VQ>? MlWwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB3NUG1NVUoRjNyNUWxOVE2RC:jPh?=
U2OS cells MYHGeY5kfGmxbjDhd5NigQ>? NGLHU|gyKM7:TR?= M1TxSm1GUzF4MjDicI9kc2WmIFXST{Bi[3SrdnH0bY9vKCiyLVXST|EwOiliaX6gR3o1OTVvdILlZZRm\CCXMl;TJINmdGy| NX3oTIRVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxN|czPDFpPkK5NVM4OjRzPD;hQi=>
CHP-212 NIL4fJBE\WyuII\pZYJqdGm2eTDhd5NigQ>? MUixNlDDqGh? MmnyTWM2OD1yLkCwPFMh|ryP NXLDRW91RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[5NlU5PDFpPkK2PVI2QDRzPD;hQi=>
SK-N-AS NF\I[GNE\WyuII\pZYJqdGm2eTDhd5NigQ>? NV23e5FzOTJywrDo MYPJR|UxRTBwME[3JO69VQ>? MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjl{NUi0NUc,OjZ7MkW4OFE9N2F-
SK-N-BE(2) MmCwR4VtdCC4aXHibYxqfHliYYPzZZk> MU[xNlDDqGh? MYfJR|UxRTBwMkig{txO NVnxNHNsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[5NlU5PDFpPkK2PVI2QDRzPD;hQi=>
SJ-NB-10 Ml\RR4VtdCC4aXHibYxqfHliYYPzZZk> NWTze3J1OTJywrDo M37VXWlEPTB;MT6xOkDPxE1? NX:yPFgxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[5NlU5PDFpPkK2PVI2QDRzPD;hQi=>
CHP-134 Mo\DR4VtdCC4aXHibYxqfHliYYPzZZk> M{DqfVEzOMLiaB?= NH3iepBKSzVyPkG1JO69VQ>? NVHwcXlJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[5NlU5PDFpPkK2PVI2QDRzPD;hQi=>
Kelly NWDnRlhSS2WubDD2bYFjcWyrdImgZZN{[Xl? NX7i[GZXOTJywrDo NH\Dfo1KSzVyPkG1JO69VQ>? M{HmRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OUK1PFQyLz5{NkmyOVg1OTxxYU6=
LAN-5 MYHD[YxtKH[rYXLpcIl1gSCjc4PhfS=> M2jTW|EzOMLiaB?= NIHvdFZKSzVyPkG1JO69VQ>? MnTLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ7MkW4OFEoRjJ4OUK1PFQyRC:jPh?=
NGP NXfHNmE6S2WubDD2bYFjcWyrdImgZZN{[Xl? NXXYeZpkOTJywrDo M4SyXmlEPTB-MUWg{txO M3jBT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OUK1PFQyLz5{NkmyOVg1OTxxYU6=
SK-N-DZ MXrD[YxtKH[rYXLpcIl1gSCjc4PhfS=> MVixNlDDqGh? NIO4T|RKSzVyPkG1JO69VQ>? M2jqSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OUK1PFQyLz5{NkmyOVg1OTxxYU6=
A549 MWDD[YxtKGO7Y3zlJIF{e2G7 MlG1NEwhOC53LDCxJO69VQ>? NH[2S4U1QGh? NYPQRnpF[XRicnXsZZRqfmWueTDsc5ch[2:wY3XueJJifGmxbjDyZY5o\XNi4pokJFEh|ryPIDjlMocvNCByLkWgZY5lKDFizszNLUBqdmS3Y3XkJGcyKGG{cnXzeC=> MorSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7M{eyPVkoRjJ3OUO3Nlk6RC:jPh?=
H157 NEf1dJBE\WyuIHP5Z4xmKGG|c3H5 NHzWepcxNCByLkWsJFEh|ryP MnPTOFhp MX\heEBz\WyjdHn2[Yx6KGyxdzDjc45k\W62cnH0bY9vKHKjbnfld{DjkaRiMTFOwG0hMGVwZz6sJFAvPSCjbnSgNUDPxE1rIHnu[JVk\WRiR{GgZZJz\XO2 M4W5eVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUO3Nlk6Lz5{NUmzO|I6QTxxYU6=
H522 MmGxR4VtdCCleXPs[UBie3OjeR?= NGHXRoIxNCByLkWsJFEh|ryP MV:0PIg> NXPBNIVM[XRicnXsZZRqfmWueTDsc5ch[2:wY3XueJJifGmxbjDyZY5o\XNi4pokJFEh|ryPIDjlMocvNCByLkWgZY5lKDFizszNLUBqdmS3Y3XkJGcyKGG{cnXzeC=> M1LhRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUO3Nlk6Lz5{NUmzO|I6QTxxYU6=
Assay
Methods Test Index PMID
Western blot MEK / p-MEK / ERK / p-ERK ; p-KIT / KIT / ETV1 26925841 25572173
Growth inhibition assay Cell viability 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 (from reference)

Animal Research:[4]
  • 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 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)F)C(=O)NOCCO

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

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%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04965818 Not yet recruiting Drug: Futibatinib and Binimetinib Advanced or Metastatic Solid Tumors Irrespective of Gene Alterations|Non-Small Cell Lung Cancer|KRAS Gene Mutation Taiho Oncology Inc. July 2021 Phase 1|Phase 2
NCT04657991 Recruiting Drug: Encorafenib|Drug: Binimetinib|Drug: Pembrolizumab Melanoma Pfizer|Merck Sharp & Dohme Corp. January 15 2021 Phase 3
NCT04543188 Recruiting Drug: PF-07284890|Drug: Binimetinib|Drug: Midazolam Malignant Melanoma|Carcinoma Non-Small-Cell Lung|Brain Neoplasms Primary|Brain Neoplasms|Malignant Neoplasms Pfizer January 8 2021 Phase 1
NCT03878719 Recruiting Drug: binimetinib|Drug: encorafenib Melanoma Pfizer|Pierre Fabre Laboratories August 13 2020 Phase 1
NCT04720768 Recruiting Drug: Binimetinib|Drug: Encorafenib|Drug: Palbociclib Melanoma|Metastasis Peter MacCallum Cancer Centre Australia June 4 2020 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2021-09-06)

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

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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.

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