Binimetinib (MEK162)

Catalog No.S7007 Batch:S700705

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Technical Data

Formula

C17H15BrF2N4O3
Molecular Weight 441.23 CAS No. 606143-89-9
Solubility (25°C)* In vitro DMSO 88 mg/mL (199.44 mM)
Water Insoluble
Ethanol Insoluble
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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]
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 Study:

[4]
  • Animal Models

    immunodeficient mice injected with MCF7-RSK4 cells.

  • Dosages

    6 mg/kg

  • Administration

    oral

Customer Product Validation

Data from [Data independently produced by , , Clin Cancer Res, 2017, 23(20):6203-6214]

Data from [Data independently produced by , , Eur J Cancer, 2018, 89:90-101]

Data from [Data independently produced by , , Oncotarget, 2016, 7(50):82185-82199]

Data from [Data independently produced by , , Tumor Biol, 2015, 36: 5699-06]

Selleck's Binimetinib (MEK162) has been cited by 94 publications

Dual Inhibition of CDK4/6 and XPO1 Induces Senescence With Acquired Vulnerability to CRBN-Based PROTAC Drugs [ Gastroenterology, 2024, S0016-5085(24)00062-3] PubMed: 38262581
Combined RAF and MEK Inhibition to Treat Activated Non-V600 BRAF-Altered Advanced Cancers [ Oncologist, 2024, 29(1):15-24] PubMed: 37616543
N-acetylcysteine overcomes NF1 loss-driven resistance to PI3Kα inhibition in breast cancer [ Cell Rep Med, 2023, 4(4):101002] PubMed: 37044095
Drug-repurposing screen on patient-derived organoids identifies therapy-induced vulnerability in KRAS-mutant colon cancer [ Cell Rep, 2023, 42(4):112324] PubMed: 37000626
SHP2 inhibitors maintain TGFβ signalling through SMURF2 inhibition [ NPJ Precis Oncol, 2023, 7(1):136] PubMed: 38102334
High-Throughput Functional Evaluation of MAP2K1 Variants in Cancer [ Mol Cancer Ther, 2023, 22(2):227-239] PubMed: 36442478
Kinome profiling identifies MARK3 and STK10 as potential therapeutic targets in uveal melanoma [ J Biol Chem, 2023, S0021-9258(23)02446-8] PubMed: 37923138
Identifying Potential Molecular Targets in Fungi Based on (Dis)Similarities in Binding Site Architecture with Proteins of the Human Pharmacolome [ Molecules, 2023, 28(2)692] PubMed: 36677748
Neuronal differentiation drives the antitumor activity of mitogen-activated protein kinase kinase (MEK) inhibition in glioblastoma [ Neurooncol Adv, 2023, 5(1):vdad132] PubMed: 38130900
Topical therapy for regression and melanoma prevention of congenital giant nevi [ Cell, 2022, S0092-8674(22)00472-X] PubMed: 35561684

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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