Binimetinib (MEK162, ARRY-162, ARRY-438162)

Catalog 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. Phase 3.

Price Stock Quantity  
USD 97 In stock
USD 370 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

Binimetinib (MEK162, ARRY-162, ARRY-438162) Chemical Structure

Binimetinib (MEK162, ARRY-162, ARRY-438162) Chemical Structure
Molecular Weight: 441.23

Validation & Quality Control

2 customer reviews :

Quality Control & MSDS

Product Information

  • Compare MEK Inhibitors
    Compare MEK Products
  • Research Area
  • Combination Therapy
    Combination Therapy

Product Description

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. Phase 3.
Targets MEK [1]
IC50 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]
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]
Features

Protocol(Only for Reference)

Animal Study: [4]

Animal Models immunodeficient mice injected with MCF7-RSK4 cells.
Formulation 0.5% Tween-80, 1% carboxymethyl cellulose
Dosages 6 mg/kg
Administration oral

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] J Pheneger, et al. 2006, ACR Annual Scientific Meeting. Abst 794.

[2] D Wright, et al. 2009, Arraybiopharma. Abstract FRI0063.

view more

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-06-25)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02185690 Withdrawn Carcinoma of the Lung. University Health Network, Toronto|Novartis Pharmaceuticals November 2016 Phase 1
NCT02631447 Not yet recruiting Metastatic Melanoma Fondazione Melanoma Onlus|Clinical Research Technology July 2016 Phase 2
NCT02451865 Not yet recruiting Recurrent Non-Small Cell Lung Carcinoma|Stage IV Non-Small Cell Lung Cancer Jonsson Comprehensive Cancer Center|National Cancer Insti  ...more Jonsson Comprehensive Cancer Center|National Cancer Institute (NCI) June 2016 Phase 1
NCT02613650 Recruiting Advanced KRAS Positive Metastatic Colorectal Cancer University of Utah|Array BioPharma May 2016 Phase 1
NCT02773459 Recruiting Biliary Tract Cancer Seoul National University Hospital April 2016 Phase 1|Phase 2

view more

Chemical Information

Download Binimetinib (MEK162, ARRY-162, ARRY-438162) SDF
Molecular Weight (MW) 441.23
Formula

C17H15BrF2N4O3

CAS No. 606143-89-9
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 88 mg/mL warming (199.44 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 1% CMC+0.5% Tween-80 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name 1H-Benzimidazole-6-carboxamide, 5-[(4-bromo-2-fluorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-

Customer Product Validation(2)


Click to enlarge
Rating
Source Tumor Biol, 2015, 36: 5699-06. Binimetinib (MEK162, ARRY-162, ARRY-438162) purchased from Selleck
Method Western Blot
Cell Lines H460 cells
Concentrations 1 µM
Incubation Time 8 h
Results Similar signaling results were also observed in H460 cells, while perifosine and MEK-162 co-treatment blocked MEK-ERK and mTORC1 activation.

Click to enlarge
Rating
Source Tumor Biol, 2015, 36: 5699-06. Binimetinib (MEK162, ARRY-162, ARRY-438162) purchased from Selleck
Method FACS Assay & ELISA Assay
Cell Lines H460 cells
Concentrations 1 µM
Incubation Time 48 h
Results Similar synergism of the two agents in activating cell apoptosis was also observed in H460 cells.

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.

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

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related MEK Products

  • Cobimetinib (GDC-0973, RG7420)

    Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM. Phase 3.

  • BI-847325

    BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.

  • GDC-0623

    GDC-0623 is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.

  • Trametinib (GSK1120212)

    Trametinib (GSK1120212) is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assays, no inhibition of the kinase activities of c-Raf, B-Raf, ERK1/2.

    Features:More potent than PD0325901 or AZD6244.

  • PD0325901

    PD0325901 is a selective and non ATP-competitive MEK inhibitor with IC50 of 0.33 nM in cell-free assays, roughly 500-fold more potent than CI-1040 on phosphorylation of ERK1 and ERK2. Phase 2.

  • Selumetinib (AZD6244)

    Selumetinib (AZD6244) is a potent, highly selective MEK1 inhibitor with IC50 of 14 nM in cell-free assays, also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Phase 3.

    Features:First MEK inhibitor being tested in Phase II clinical trials.

  • U0126-EtOH

    U0126-EtOH is a highly selective inhibitor of MEK1/2 with IC50 of 0.07 μM/0.06 μM in cell-free assays, 100-fold higher affinity for ΔN3-S218E/S222D MEK than PD98059.

    Features:A chemically synthesized and highly selective inhibitor of both MEK1 and MEK2.

  • PD98059

    PD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 μM in a cell-free assay, specifically inhibits MEK-1-mediated activation of MAPK; does not directly inhibit ERK1 or ERK2.

    Features:Does not inhibit c-Raf phosphorylated MEK1.

  • PD184352 (CI-1040)

    PD184352 (CI-1040) is an ATP non-competitive MEK1/2 inhibitor with IC50 of 17 nM in cell-based assays, 100-fold more selective for MEK1/2 than MEK5. Phase 2.

    Features:First MEK inhibitor to begin clinical development.

  • Refametinib (RDEA119, Bay 86-9766)

    Refametinib (RDEA119, Bay 86-9766) is a potent, ATP non-competitive and highly selective inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively.

Recently Viewed Items

Tags: buy Binimetinib (MEK162, ARRY-162, ARRY-438162) | Binimetinib (MEK162, ARRY-162, ARRY-438162) supplier | purchase Binimetinib (MEK162, ARRY-162, ARRY-438162) | Binimetinib (MEK162, ARRY-162, ARRY-438162) cost | Binimetinib (MEK162, ARRY-162, ARRY-438162) manufacturer | order Binimetinib (MEK162, ARRY-162, ARRY-438162) | Binimetinib (MEK162, ARRY-162, ARRY-438162) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Contact Us