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Binimetinib (MEK162) MEK inhibitor

Name: Binimetinib (MEK162)
SKU: S7007
Availability: InStock
Rating: 5 (105 reviews)

Cat.No.S7007

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

Chemical Structure

Molecular Weight: 441.23

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	Ras ERK p38 MAPK Raf JNK S6 Kinase MAP4K TAK1 Mixed Lineage Kinase ASK MNK MAPKAPK2 KLF TOPK
Related Products	Mirdametinib (PD0325901) U0126-EtOH PD98059 PD184352 (CI-1040) BIX 02189 Pimasertib (AS-703026) Refametinib (RDEA119) TAK-733 AZD8330 BIX 02188 GDC-0623 SL-327 Myricetin BI-847325 PD318088 APS-2-79 HCl MEK1 Antibody [F9N7] PD184161 Nedometinib MEK1 Antibody [G24C19] GW284543 (UNC10225170) RO4987655 Atebimetinib (IMM-1-104) MEK1/2 Antibody [J11P23] Zapnometinib (PD0184264) Tunlametinib Phospho-MEK1/2 (Ser217/221) Antibody [G6P21] Rap1B Antibody [H22K21] MEK2 Antibody [M18L8] Rap1A/Rap1B Antibody [E5J15]

Cell Culture, Treatment & Working Concentration

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

Chemical Information, Storage & Stability

Molecular Weight	441.23	Formula	C₁₇H₁₅BrF₂N₄O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	606143-89-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	ARRY-162,ARRY-438162			Smiles	CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)F)C(=O)NOCCO

Solubility

In vitro
Batch:

DMSO : 88 mg/mL (199.44 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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+ %

Calculation results:

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.

Mechanism of Action

Targets/IC₅₀/Ki	MEK ^[1] (Cell-free assay) 12 nM
In vitro	Binimetinib (MEK162) is a recently disclosed potent and selective ATP non-competitive MEK1/2 inhibitor, inhibits pERK in cells with an IC50 of11 nM. ^[3] This compound (625 nM) inhibits in vitro osteoclast differentiation with IC50 of 39 nM. It (10 μM) inhibits in vitro osteoclast resorption with IC50 of 625 nM. It (2 μM) weakly affects osteoblast differentiation. ^[2] It (1 μM) combined with MK-2206 (2 μM) completely reverses the resistance of RSK-expressing MCF7 cells. ^[4]
In vivo	Binimetinib (MEK162) 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. This compound also shows 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. At 30 mg/kg, it demonstrates dose-related inhibition of relative spleen weights in rat adjuvant-induced arthritis (AIA) models. Additionally, it significantly inhibits bone resorption and inflammation with delayed dosing when compared to vehicle in rat adjuvant-induced arthritis (AIA) models. ^[2] 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. It (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. It inhibits AIA ankle diameter 11% and 34% at 3 mg/kg and 10 mg/kg in rat adjuvant-induced arthritis (AIA) models. ^[1] When combined with BEZ235, it (6 mg/kg, BID) results in a significant reduction of tumor growth in immunodeficient mice injected with MCF7 cells. ^[4]
References	[1] https://acr.confex.com/acr/2006/webprogram/Paper5558.html [2] http://www.arraybiopharma.com/_documents/Publication/PubAttachment349.pdf [3] http://www.sciencedirect.com/science/article/pii/S0065774307420176 [4] https://pubmed.ncbi.nlm.nih.gov/23635776/ [5] https://pubmed.ncbi.nlm.nih.gov/32442403/

Applications

Methods	Biomarkers	Images	PMID
Western blot	MEK / p-MEK / ERK / p-ERK p-KIT / KIT / ETV1		26925841
Growth inhibition assay	Cell viability		26925841

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

Question 1:
Could you please clarify whether the formulation in vivo for S7007 is clear or not?

Answer:
It can be dissolved in 5% DMSO+45% PEG 300+ddH2O at 5 mg/ml clearly for injection.

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