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 74 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 Mk\2SpVv[3Srb36gZZN{[Xl? MlXYTWM2OD1zMUWgcm0> MlruQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|NUK1OlUoRjNyM{WyOVY2RC:jPh?=
Mel IL NHHoVJlEgXSxdH;4bYNqfHliYYPzZZk> NEHKXIRKSzVyPUOuO{DDuSByLkKg{txO M3jzdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNUWxOVE2Lz5|MEW1NVUyPTxxYU6=
Mel IL/R MVXDfZRwfG:6aXPpeJkh[XO|YYm= MXfJR|UxRTJwNzFCtUAxNjNizszN MmDTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB3NUG1NVUoRjNyNUWxOVE2RC:jPh?=
Mel Z NXPwbZg4S3m2b4TvfIlkcXS7IHHzd4F6 MmXuTWM2OD1|LkigxtEhOC5{IN88US=> M2L5T|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNUWxOVE2Lz5|MEW1NVUyPTxxYU6=
A375 M{C3eGN6fG:2b4jpZ4l1gSCjc4PhfS=> MmPCTWM2OD17LkigxtEhOC5zIN88US=> NUfO[|J6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C1OVE2OTVpPkOwOVUyPTF3PD;hQi=>
Mel Me NW\INmY1S3m2b4TvfIlkcXS7IHHzd4F6 MVjJR|UxRTF|LkOgxtEhOC5|IN88US=> Ml[1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB3NUG1NVUoRjNyNUWxOVE2RC:jPh?=
Mel MTP M1rib2N6fG:2b4jpZ4l1gSCjc4PhfS=> NUTOV3EyUUN3ME2xNE4zKMLzIECuOEDPxE1? MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODV3MUWxOUc,OzB3NUG1NVU9N2F-
U2OS cells NFrC[WVHfW6ldHnvckBie3OjeR?= M4Sxb|Eh|ryP MXfNSWsyPjJiYnzvZ4tm\CCHUlugZYN1cX[jdHnvckApeC2HUluxM|IqKGmwIFPaOFE2NXS{ZXH0[YQhXTKRUzDj[Yxtew>? M4DhcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUO3NlQyLz5{OUGzO|I1OTxxYU6=
CHP-212 NXW5RnRwS2WubDD2bYFjcWyrdImgZZN{[Xl? M2\RTlEzOMLiaB?= NHHKWYFKSzVyPUCuNFA5OyEQvF2= MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjl{NUi0NUc,OjZ7MkW4OFE9N2F-
SK-N-AS Mk\kR4VtdCC4aXHibYxqfHliYYPzZZk> MV:xNlDDqGh? NFq1bpVKSzVyPUCuNFY4KM7:TR?= MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjl{NUi0NUc,OjZ7MkW4OFE9N2F-
SK-N-BE(2) NHHQOHFE\WyuII\pZYJqdGm2eTDhd5NigQ>? NVLqN4pWOTJywrDo NVuxfYJoUUN3ME2wMlI5KM7:TR?= NWraNmk3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[5NlU5PDFpPkK2PVI2QDRzPD;hQi=>
SJ-NB-10 Mo\0R4VtdCC4aXHibYxqfHliYYPzZZk> Mnf2NVIxyqCq NXnybphpUUN3ME2xMlE3KM7:TR?= MnzmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ7MkW4OFEoRjJ4OUK1PFQyRC:jPh?=
CHP-134 NYHGPWdTS2WubDD2bYFjcWyrdImgZZN{[Xl? NHr4ZnoyOjEEoHi= MlfDTWM2OD5zNTFOwG0> MkPjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ7MkW4OFEoRjJ4OUK1PFQyRC:jPh?=
Kelly M{jD[WNmdGxidnnhZoltcXS7IHHzd4F6 MoLWNVIxyqCq M1zrTGlEPTB-MUWg{txO MnfMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ7MkW4OFEoRjJ4OUK1PFQyRC:jPh?=
LAN-5 NFnBNmtE\WyuII\pZYJqdGm2eTDhd5NigQ>? NF7BXI4yOjEEoHi= MUPJR|UxRjF3IN88US=> MkfXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ7MkW4OFEoRjJ4OUK1PFQyRC:jPh?=
NGP M1HlZWNmdGxidnnhZoltcXS7IHHzd4F6 M{XETVEzOMLiaB?= NF\KeVhKSzVyPkG1JO69VQ>? NFPhN3g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkmyOVg1OSd-Mk[5NlU5PDF:L3G+
SK-N-DZ NXvnfmdES2WubDD2bYFjcWyrdImgZZN{[Xl? MYWxNlDDqGh? Mn3tTWM2OD5zNTFOwG0> MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjl{NUi0NUc,OjZ7MkW4OFE9N2F-
A549 NXvFe2VtS2WubDDjfYNt\SCjc4PhfS=> NVjhcZUyOCxiMD61MEAyKM7:TR?= M3nyblQ5cA>? NUXldHVq[XRicnXsZZRqfmWueTDsc5ch[2:wY3XueJJifGmxbjDyZY5o\XNi4pokJFEh|ryPIDjlMocvNCByLkWgZY5lKDFizszNLUBqdmS3Y3XkJGcyKGG{cnXzeC=> Mmf4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7M{eyPVkoRjJ3OUO3Nlk6RC:jPh?=
H157 Ml\MR4VtdCCleXPs[UBie3OjeR?= Mn3aNEwhOC53LDCxJO69VQ>? MYK0PIg> M{XNWoF1KHKnbHH0bZZmdHlibH;3JINwdmOnboTyZZRqd25icnHu[4V{KOLLpDCxJO69VSBqZT7nMkwhOC53IHHu[EAyKM7:TTmgbY5lfWOnZDDHNUBienKnc4S= NVTI[phXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5N|czQTlpPkK1PVM4Ojl7PD;hQi=>
H522 MkLLR4VtdCCleXPs[UBie3OjeR?= NFW2WnYxNCByLkWsJFEh|ryP NWGzSFliPDiq NInVZ29ifCC{ZXzheIl3\Wy7IHzve{Bkd26lZX70doF1cW:wIILhcodmeyEkibSgNUDPxE1iKHWu[{4tKDBwNTDhcoQhOSEQvF2pJIlv\HWlZXSgS|Eh[XK{ZYP0 NXvKT4l5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5N|czQTlpPkK1PVM4Ojl7PD;hQi=>
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

Solubility (25°C)

In vitro

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

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)

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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.
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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05080621 Withdrawn Drug: Ripretinib|Drug: binimetinib Gastrointestinal Stromal Tumors Deciphera Pharmaceuticals LLC November 2021 Phase 1|Phase 2
NCT04965818 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. September 20 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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

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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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