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Binimetinib

SKU: orb1305378

Description

Binimetinib (ARRY-162) is an orally bioavailable, selective MEK1/2 inhibitor (IC50=12 nM). It exhibits antitumor activity and is used in research for unresectable or BRAF V600E/K mutant metastatic melanoma. Its application extends to in vitro signaling studies and in vivo xenograft models investigating MAPK pathway inhibition.

Research Area

Cell Biology, Signal Transduction

Images & Validation

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Binimetinib

Key Properties

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CAS Number606143-89-9
MW441.23
Purity99.00%
FormulaC17H15BrF2N4O3
SMILESCn1cnc2c(F)c(Nc3ccc(Br)cc3F)c(cc12)C(=O)NOCCO
TargetMEK,Autophagy
SolubilityEthanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:50 mg/mL (113.32 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.53 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

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Target IC50
MEK:12 nM
In Vivo
ARRY-438162 is an ATP non-competitive inhibitor for MEK1/2, capable of inhibiting intracellular pERK with an IC50 of 11 nM. When used in combination, MEK162 (1 μM) and MK-2206 (2 μM) can fully reverse the resistance of MCF7 cells expressing RSK. ARRY-438162 at 2 μM exhibits minimal impact on osteoblast differentiation. At a concentration of 10 μM, ARRY-438162 inhibits osteoclast resorption in vitro with an IC50 of 625 nM. Additionally, ARRY-438162 at 625 nM suppresses osteoclast differentiation in vitro with an IC50 of 39 nM.
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In Vitro
In models of collagen-induced arthritis (CIA) and adjuvant-induced arthritis (AIA) in rats, ARRY-438162 demonstrated significant anti-inflammatory effects. At doses of 1/3 mg/kg administered twice daily orally (p.o.), ARRY-438162 reduced ankle diameter swelling by 27%/50% in the CIA model, outperforming ibuprofen's 46% reduction. Higher doses of 3/10 mg/kg showed 11%/34% inhibition of ankle swelling in the AIA model. Moreover, in immunodeficient mice injected with MCF7-RSK4 cells, the combination of ARRY-438162 (6 mg/kg, twice daily) with BEZ235 significantly diminished tumor growth. In the AIA rat model, ARRY-438162 (10 mg/kg) completely suppressed serum IL-6 concentrations in a dose-dependent manner compared to controls. Similarly, in both CIA and AIA rat models, administration of ARRY-438162 (10 mg/kg, twice daily p.o.) dose-dependently ameliorated disease severity. The same dosing regimen significantly mitigated lesions (inflammation, cartilage damage, angiogenesis, and bone resorption) in the CIA model, with 1/3 mg/kg doses inhibiting these effects by 32% and 60%, respectively. Furthermore, in the AIA rat model, ARRY-438162 at 10/30 mg/kg doses significantly and dose-dependently reduced ankle swelling compared to control groups.
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Cell Research
MEK162 is dissolved in DMSO and stored, and then diluted with appropriate medium before use. MCF7 cells infected as indicated are seeded in 12-well plates (2×104). After 24 hours, cells are treated with BEZ235 (100 or 200 nM), BKM120 (0.75 or 1 μM), GDC-0941 (1 μM), or MK2206 (2 μM) alone or in combination with MEK162 (1 μM), BI-D1870 (10 μM), or AZD6244 (1 μM), as indicated in text. Cell numbers are quantified by fixing cells with 4% glutaraldehyde or methanol, washing the cells twice in Water, and staining the cells with 0.1% crystal violet. The dye is subsequently extracted with 10% acetic acid, and its absorbance is determined (570 nm). Growth curves are performed in triplicate. Viability assays with CellTiter-Glo are performed by plating 2,000 cells in 96-well plates, adding the drug at 24 hours, and assaying 4 to 5 days after drug addition. Cell-cycle and hypodiploid apoptotic cells are quantified by flow cytometry. Briefly, cells are washed with PBS, fixed in cold 70% ethanol, and then stained with propidium iodide while being treated with RNase. Quantitative analysis of sub-G1 cells is carried out in a FACScalibur cytometer using Cell Quest software.
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Storage & Handling

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StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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Inhibitor, inhibit, Mitogen-activated protein kinase kinase, MAP2K, MAPKK, MEK162, MEK-162, MEK 162, MEK, Autophagy, ARRY 162, ARRY438162, ARRY-438162, ARRY 438162, ARRY162, ARRY-162, Binimetinib

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Compound Identifiers

PubChem CID
10288191 ↗

Key Properties

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No computed properties available.

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Binimetinib (orb1305378)

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% DMSO +
%+
% Tween 80 +
%

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5 mg
$ 80.00
10 mg
$ 100.00
1 ml x 10 mM (in DMSO)
$ 110.00
25 mg
$ 110.00
50 mg
$ 120.00
100 mg
$ 140.00
200 mg
$ 200.00
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