Binimetinib (MEK162)

別名:ARRY-162,ARRY-438162

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.

Binimetinib (MEK162)化学構造

CAS No. 606143-89-9

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 15900 国内在庫あり
JPY 18100 国内在庫あり
JPY 63400 国内在庫あり
JPY 118700 国内在庫あり
JPY 187800 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(90)

製品安全説明書

現在のバッチを見る: 純度: 99.98%
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Binimetinib (MEK162)と併用されることが多い化合物

Trametinib (GSK1120212)


Binimetinib and Trametinib subcutaneous injection result in hypopigmentation and almost complete loss of melanocytes.

Choi YS, et al. Cell. 2022 Jun 9;185(12):2071-2085.e12.

Cobimetinib (GDC-0973)


Binimetinib and Cobimetinib are MEK 1 inhibitors that are FDA-approved together with RAF inhibitors to treat BRAF V600 mutant melanoma.

Gao Y, et al. Cancer Discov. 2019 Sep;9(9):1182-1191.

Encorafenib


Binimetinib and Encorafenib is the third BRAF plus MEK inhibitor combination to be approved.

Davis J, et al. J Adv Pract Oncol. 2022 May;13(4):450-455.

Selumetinib (AZD6244)


Selumetinib is the only licensed medical therapy for NF1-PN pediatric patients, whereas binimetinib is being investigated as a medical therapy for NF1-PN.

Armstrong AE, et al. BMC Cancer. 2023 Jun 16;23(1):553.

Binimetinib (MEK162)関連製品

シグナル伝達経路

MEK阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
A549 Cell cycle assay 0, 0.5, 1 μM 48h at relatively low concentration ranges ≤ 1 μM (e.g., 0.5 and 1 μM) induced G1 arrest 25937299
H157 Cell cycle assay 0, 0.5, 1 μM 48h at relatively low concentration ranges ≤ 1 μM (e.g., 0.5 and 1 μM) induced G1 arrest 25937299
H522 Cell cycle assay 0, 0.5, 1 μM 48h at relatively low concentration ranges ≤ 1 μM (e.g., 0.5 and 1 μM) induced G1 arrest 25937299
U2OS cells Function assay 1 μM MEK162 blocked ERK activation (p-ERK1/2) in CZ415-treated U2OS cells 29137241
SK-N-BE(2) Cell viability assay 120 h IC50=0.28 μM 26925841
SK-N-AS Cell viability assay 120 h IC50=0.067 μM 26925841
CHP-212 Cell viability assay 120 h IC50=0.0083 μM 26925841
SJ-NB-10 Cell viability assay 120 h IC50=1.16 μM 26925841
CHP-134 Cell viability assay 120 h IC50>15 μM 26925841
Kelly Cell viability assay 120 h IC50>15 μM 26925841
LAN-5 Cell viability assay 120 h IC50>15 μM 26925841
NGP Cell viability assay 120 h IC50>15 μM 26925841
SK-N-DZ Cell viability assay 120 h IC50>15 μM 26925841
Mel MTP Cytotoxicity assay IC50=10.2 ± 0.4 μM 30551515
Mel Me Cytotoxicity assay IC50=13.3 ± 0.3 μM 30551515
A375 Cytotoxicity assay IC50=9.8 ± 0.1 μM 30551515
Mel Z Cytotoxicity assay IC50=3.8 ± 0.2 μM 30551515
Mel IL/R Cytotoxicity assay IC50=2.7 ± 0.3 μM 30551515
Mel IL Cytotoxicity assay IC50=3.7 ± 0.2 μM 30551515
NCI-H727 Function assay IC50=115 nM 30352565
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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.
Targets
MEK [1]
(Cell-free assay)
12 nM
In Vitro
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]

実験結果図 Methods Biomarkers 結果図 PMID
Western blot p-KIT / KIT / ETV1 MEK / p-MEK / ERK / p-ERK 25572173
Growth inhibition assay Cell viability 26925841
In Vivo
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]

動物実験 動物モデル immunodeficient mice injected with MCF7-RSK4 cells.
投与量 6 mg/kg
投与経路 oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05286788 Recruiting
Adamantinous Craniopharyngioma|Recurrent Adamantinomatous Craniopharyngioma
Nationwide Children''s Hospital|Children''s Hospital Colorado
April 10 2023 Phase 2
NCT05810740 Completed
Melanoma|BRAF V600 Mutation|Unresectable Melanoma|Metastatic Melanoma
Pierre Fabre Medicament|Biotrial
August 31 2022 Phase 1
NCT05195632 Active not recruiting
Non-Small Cell Lung Cancer
Pierre Fabre Medicament
June 2 2022 Phase 2
NCT05767879 Recruiting
Melanoma Stage III|In-Transit Metastasis of Cutaneous Melanoma
Leiden University Medical Center|Pierre Fabre Laboratories
January 1 2022 Phase 2
NCT05080621 Withdrawn
Gastrointestinal Stromal Tumors
Deciphera Pharmaceuticals LLC
November 2021 Phase 1|Phase 2

化学情報

分子量 441.23 化学式

C17H15BrF2N4O3

CAS No. 606143-89-9 SDF Download Binimetinib (MEK162) SDFをダウンロードする
Smiles CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)F)C(=O)NOCCO
保管

In vitro
Batch:

DMSO : 88 mg/mL ( (199.44 mM); Warmed with 50℃ water bath; 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

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Handling Instructions

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よくある質問(FAQ)

質問1:
Could please clarify the formulation in vivo for S7007 is clear or not?

回答
S7007 can be dissolved in 5% DMSO+45% PEG 300+ddH2O at 5 mg/ml clearly for injection.

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