Home MAPK MEK inhibitor - Autophagy activator - Apoptosis related activator Binimetinib (MEK162) For research use only.

Binimetinib (MEK162)

Synonyms: ARRY-162,ARRY-438162

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

Binimetinib (MEK162) Chemical Structure

CAS No. 606143-89-9

Purity & Quality Control

Binimetinib (MEK162) Related Products

Signaling Pathway

MEK Signaling Pathways

MEK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H727 Function assay IC50=115 nM 30352565
Mel IL Cytotoxicity assay IC50=3.7 ± 0.2 μM 30551515
Mel IL/R Cytotoxicity assay IC50=2.7 ± 0.3 μM 30551515
Mel Z Cytotoxicity assay IC50=3.8 ± 0.2 μM 30551515
A375 Cytotoxicity assay IC50=9.8 ± 0.1 μM 30551515
Mel Me Cytotoxicity assay IC50=13.3 ± 0.3 μM 30551515
Mel MTP Cytotoxicity assay IC50=10.2 ± 0.4 μM 30551515
U2OS cells Function assay 1 μM MEK162 blocked ERK activation (p-ERK1/2) in CZ415-treated U2OS cells 29137241
CHP-212 Cell viability assay 120 h IC50=0.0083 μM 26925841
SK-N-AS Cell viability assay 120 h IC50=0.067 μM 26925841
SK-N-BE(2) Cell viability assay 120 h IC50=0.28 μM 26925841
SJ-NB-10 Cell viability assay 120 h IC50=1.16 μM 26925841
CHP-134 Cell viability assay 120 h IC50>15 μM 26925841
Kelly Cell viability assay 120 h IC50>15 μM 26925841
LAN-5 Cell viability assay 120 h IC50>15 μM 26925841
NGP Cell viability assay 120 h IC50>15 μM 26925841
SK-N-DZ Cell viability assay 120 h IC50>15 μM 26925841
A549 Cell cycle assay 0, 0.5, 1 μM 48h at relatively low concentration ranges ≤ 1 μM (e.g., 0.5 and 1 μM) induced G1 arrest 25937299
H157 Cell cycle assay 0, 0.5, 1 μM 48h at relatively low concentration ranges ≤ 1 μM (e.g., 0.5 and 1 μM) induced G1 arrest 25937299
H522 Cell cycle assay 0, 0.5, 1 μM 48h at relatively low concentration ranges ≤ 1 μM (e.g., 0.5 and 1 μM) induced G1 arrest 25937299
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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
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]
Experimental Result Images Methods Biomarkers Images PMID
Western blot MEK / p-MEK / ERK / p-ERK p-KIT / KIT / ETV1 26925841
Growth inhibition assay Cell viability 26925841
In Vivo
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 Animal Models immunodeficient mice injected with MCF7-RSK4 cells.
Dosages 6 mg/kg
Administration oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06207656 Not yet recruiting
Colorectal Cancer
Spanish Cooperative Group for the Treatment of Digestive Tumours (TTD)|Merck S.L. Spain|Pierre Fabre Ibérica S.A.
 January 19 2024 Phase 2
NCT05286788 Recruiting
Adamantinous Craniopharyngioma|Recurrent Adamantinomatous Craniopharyngioma
Nationwide Children''s Hospital|Children''s Hospital Colorado
 April 10 2023 Phase 2
NCT05810740 Completed
Melanoma|BRAF V600 Mutation|Unresectable Melanoma|Metastatic Melanoma
Pierre Fabre Medicament|Biotrial
 August 31 2022 Phase 1
NCT05195632 Active not recruiting
Non-Small Cell Lung Cancer
Pierre Fabre Medicament
 June 2 2022 Phase 2
NCT05767879 Recruiting
Melanoma Stage III|In-Transit Metastasis of Cutaneous Melanoma
Leiden University Medical Center|Pierre Fabre Laboratories
 January 1 2022 Phase 2

Chemical Information & Solubility

Molecular Weight 441.23 Formula

C17H15BrF2N4O3
CAS No. 606143-89-9 SDF Download Binimetinib (MEK162) SDF
Smiles CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)F)C(=O)NOCCO
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 88 mg/mL ( (199.44 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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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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