Binimetinib (MEK162)

製品コードS7007 バッチS700705

印刷

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 (warmed with 50ºC water bath)

88 mg/mL (199.44 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 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.

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) 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.
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. ^[3] 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. ^[2] MEK162 (1 μM) combined with MK-2206 (2 μM) completely reverses the resistance of RSK-expressing MCF7 cells. ^[4]
in vivo	Binimetinib (MEK162) reduces disease severity in a dose-related manner in rat collagen-induced arthritis (CIA) and rat adjuvant-induced arthritis (AIA) models at 10 mg/kg (po, bid). In the rat CIA model, this compound (po, bid) inhibits increases in ankle diameter by 27% and 50% at 1 mg/kg and 3 mg/kg, while ibuprofen has 46% inhibition. It 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 same model. In rat AIA models, it inhibits ankle diameter 11% and 34% at 3 mg/kg and 10 mg/kg. ^[1] It demonstrates dose-related inhibition of ankle swelling in rat 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 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 AIA models. Additionally, it significantly inhibits bone resorption and inflammation with delayed dosing when compared to vehicle in rat AIA models at 30 mg/kg. ^[2] When combined with BEZ235 at 6 mg/kg (BID), it results in a significant reduction of tumor growth in immunodeficient mice injected with MCF7 cells. ^[4]

製品説明

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.

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. ^[3]

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. ^[2]

MEK162 (1 μM) combined with MK-2206 (2 μM) completely reverses the resistance of RSK-expressing MCF7 cells. ^[4]

in vivo

Binimetinib (MEK162) reduces disease severity in a dose-related manner in rat collagen-induced arthritis (CIA) and rat adjuvant-induced arthritis (AIA) models at 10 mg/kg (po, bid). In the rat CIA model, this compound (po, bid) inhibits increases in ankle diameter by 27% and 50% at 1 mg/kg and 3 mg/kg, while ibuprofen has 46% inhibition. It 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 same model. In rat AIA models, it inhibits ankle diameter 11% and 34% at 3 mg/kg and 10 mg/kg. ^[1]

It demonstrates dose-related inhibition of ankle swelling in rat 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 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 AIA models. Additionally, it significantly inhibits bone resorption and inflammation with delayed dosing when compared to vehicle in rat AIA models at 30 mg/kg. ^[2]

When combined with BEZ235 at 6 mg/kg (BID), it results in a significant reduction of tumor growth in immunodeficient mice injected with MCF7 cells. ^[4]

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 this compound.
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：

Combined inhibition of focal adhesion kinase and RAF/MEK elicits synergistic inhibition of melanoma growth and reduces metastases [ Cell Rep Med, 2025, 6(2):101943]	PubMed: 39922199
Geometric deep learning and multiple-instance learning for 3D cell-shape profiling [ Cell Syst, 2025, 16(3):101229]	PubMed: 40112779
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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