MEK162 (Binimetinib, ARRY-162)

製品コードS7007 バッチS700707

化学情報

	Synonyms	ARRY-162,ARRY-438162	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₇H₁₅BrF₂N₄O₃
	分子量	441.23	CAS No.	606143-89-9
Solubility (25°C)*	体外	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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Binimetinib (MEK162, ARRY-162, ARRY-438162) は、無細胞アッセイにおいて12 nMのIC50を示すMEK1/2の強力な阻害剤です。Binimetinibは、ヒトNSCLC細胞株においてG1細胞周期停止とapoptosisを誘導し、さらにautophagyを誘導します。現在フェーズ3です。
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. 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. It (1 μM) combined with MK-2206 (2 μM) completely reverses the resistance of RSK-expressing MCF7 cells.
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. 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. When combined with BEZ235, it (6 mg/kg, BID) results in a significant reduction of tumor growth in immunodeficient mice injected with MCF7 cells.

製品説明

Binimetinib (MEK162, ARRY-162, ARRY-438162) は、無細胞アッセイにおいて12 nMのIC50を示すMEK1/2の強力な阻害剤です。Binimetinibは、ヒトNSCLC細胞株においてG1細胞周期停止とapoptosisを誘導し、さらにautophagyを誘導します。現在フェーズ3です。

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.

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.

It (1 μM) combined with MK-2206 (2 μM) completely reverses the resistance of RSK-expressing MCF7 cells.

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.

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.

When combined with BEZ235, it (6 mg/kg, BID) results in a significant reduction of tumor growth in immunodeficient mice injected with MCF7 cells.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	KPCN cells
	濃度	10 nM
	反応時間
	実験の流れ	Cells were treated with indicated concentrations of Binimetinib (MEK162).
動物実験	動物モデル	immunodeficient mice injected with MCF7-RSK4 cells.
	投薬量	6 mg/kg
	投与方法	oral

参考

https://acr.confex.com/acr/2006/webprogram/Paper5558.html
http://www.arraybiopharma.com/_documents/Publication/PubAttachment349.pdf
http://www.sciencedirect.com/science/article/pii/S0065774307420176

https://pubmed.ncbi.nlm.nih.gov/23635776/
https://pubmed.ncbi.nlm.nih.gov/32442403/

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カスタマーフィードバック

: 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]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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Basroparib overcomes acquired resistance to MEK inhibitors by inhibiting Wnt-mediated cancer stemness in KRAS-mutated colorectal cancer [ Biochem Pharmacol, 2025, 235:116842]	PubMed: 40024348
Integration of focal adhesion morphogenesis and polarity by DOCK5 promotes YAP/TAZ-driven drug resistance in TNBC [ Mol Omics, 2025, 10.1039/d4mo00154k]	PubMed: 40353692
Tumour-selective activity of RAS-GTP inhibition in pancreatic cancer [ Nature, 2024, 629(8013):927-936]	PubMed: 38588697
MEK inhibition prevents CAR-T cell exhaustion and differentiation via downregulation of c-Fos and JunB [ Signal Transduct Target Ther, 2024, 9(1):293]	PubMed: 39438476
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
Nutritional vitamin B12 regulates RAS/MAPK-mediated cell fate decisions through one-carbon metabolism [ Nat Commun, 2024, 15(1):8178]	PubMed: 39289374
EHMT2 promotes tumorigenesis in GNAQ/11-mutant uveal melanoma via ARHGAP29-mediated RhoA pathway [ Acta Pharm Sin B, 2024, 14(3):1187-1203]	PubMed: 38486999
Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862]	PubMed: 39319271

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人間や獣医の診断であるか治療的な使用のためにでない。

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