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Binimetinib (MEK162)

Name: Binimetinib (MEK162)
Brand: Selleck Chemicals
SKU: S7007
Rating: 5 (91 reviews)

Synonyms: ARRY-162,ARRY-438162

Catalog No.S7007 Purity: 99.98%

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: 606143-89-9

Selleck's Binimetinib (MEK162) has been cited by 91 publications

Purity & Quality Control

Batch: Purity: 99.98%

99.98

Products often used together with Binimetinib (MEK162)

Trametinib (GSK1120212)

Binimetinib and Trametinib subcutaneous injection result in hypopigmentation and almost complete loss of melanocytes.

Choi YS, et al. Cell. 2022 Jun 9;185(12):2071-2085.e12.

Cobimetinib (GDC-0973)

Binimetinib and Cobimetinib are MEK 1 inhibitors that are FDA-approved together with RAF inhibitors to treat BRAF V600 mutant melanoma.

Gao Y, et al. Cancer Discov. 2019 Sep;9(9):1182-1191.

Encorafenib

Binimetinib and Encorafenib is the third BRAF plus MEK inhibitor combination to be approved.

Davis J, et al. J Adv Pract Oncol. 2022 May;13(4):450-455.

Selumetinib (AZD6244)

Selumetinib is the only licensed medical therapy for NF1-PN pediatric patients, whereas binimetinib is being investigated as a medical therapy for NF1-PN.

Armstrong AE, et al. BMC Cancer. 2023 Jun 16;23(1):553.

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Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	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
Click to View More Cell Line Experimental Data

Biological Activity

Description

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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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
NCT05080621	Withdrawn	Gastrointestinal Stromal Tumors	Deciphera Pharmaceuticals LLC	November 2021	Phase 1\|Phase 2

References

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Chemical lnformation & 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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

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Molarity Calculator

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Dilution Calculator Molecular Weight Calculator

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:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%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.

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.

MEK Signaling Pathway Map

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