Binimetinib (ARRY-162, MEK162) | MEK inhibitor | Probechem Biochemicals

Chemical Structure : Binimetinib

CAS No.: 606143-89-9

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

货号: PC-49771Not For Human Use, Lab Use Only.

Binimetinib (ARRY-162, ARRY-438162, MEK162) is a potent, selective and non-competitive inhibitor of MEK1/2 with IC50 of 12 nM in cell-free assays.

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10 mg	￥580	In stock
50 mg	￥1280	In stock
100 mg	￥1980	In stock
250 mg	￥3280	In stock
1 g		Get quote

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生物&药学活性

Binimetinib (ARRY-162, ARRY-438162, MEK162) is a potent, selective and non-competitive inhibitor of MEK1/2 with IC50 of 12 nM in cell-free assays.
Binimetinib (ARRY-162, ARRY-438162, MEK162) induces G1 cell cycle arrest and apoptosis in human NSCLC cell lines and induces autophagy.
Binimetinib (ARRY-162, ARRY-438162, MEK162) inhibits in vitro osteoclast differentiation with IC50 of 39 nM.
Binimetinib (ARRY-162, ARRY-438162, MEK162) (10 μM) inhibits in vitro osteoclast resorption with IC50 of 625 nM.
Binimetinib (ARRY-162, ARRY-438162, MEK162) inhibits pERK in cells with an IC50 of 11 nM.
Binimetinib (ARRY-162, ARRY-438162, MEK162) (1 μM) combined with MK-2206 (2 μM) completely reverses the resistance of RSK-expressing MCF7 cells.
Binimetinib (ARRY-162, ARRY-438162, MEK162) (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.
Binimetinib (ARRY-162, ARRY-438162, MEK162) (6 mg/kg, BID) combined with BEZ235 treatment caused a significant reduction of tumor growth in immunodeficient mice injected with MCF7 cells.

物理化学性质&存储条件

分子量	441.23
分子式	C17H15BrF2N4O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	5-((4-Bromo-2-fluorophenyl)amino)-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzo[d]imidazole-6-carboxamide

参考文献

1. Ascierto PA, et al. Lancet Oncol. 2013 Mar;14(3):249-56.

2. Gritsman K, et al. J Clin Invest. 2014 Apr;124(4):1794-809.

3. Johanna C Bendell, et al. Br J Cancer. 2017 Feb 28;116(5):575-583.

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

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

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