Trametinib

カタログ番号 T2125 CAS 871700-17-3

別名: GSK1120212, JTP-74057

Trametinib (GSK1120212) is a MEK inhibitor that inhibits MEK1 and MEK2 (IC50=0.7/0.9 nM) with ATP non-competitive and oral activity. Trametinib activates autophagy and induces apoptosis.

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Trametinib, CAS 871700-17-3

パッケージサイズ	在庫状況	単価(税別)
サンプルについてお問い合わせ
5 mg	在庫あり	￥ 7,500
10 mg	在庫あり	￥ 11,500
50 mg	在庫あり	￥ 15,000
100 mg	在庫あり	￥ 23,000
200 mg	在庫あり	￥ 32,500
1 mL * 10 mM (in DMSO)	在庫あり	￥ 11,500

バルクのお問い合わせ

バッチを選択

純度: 99.88%

COA DATASHEET SDS HPLC HNMR

純度: 99.88%

COA DATASHEET SDS HNMR HPLC

純度: 99.88%

DATASHEET SDS

純度: 99.72%

COA DATASHEET SDS HNMR HPLC

純度: 99.71%

COA DATASHEET SDS HPLC HNMR

純度: 99.39%

COA DATASHEET SDS HPLC HNMR

純度: 98%

COA DATASHEET SDS HNMR

DATASHEET SDS

バッチの詳細情報はお問い合わせください

生物学的特性に関する説明

化学的特性

保存条件 & 溶解度情報

説明	Trametinib (GSK1120212) is a MEK inhibitor that inhibits MEK1 and MEK2 (IC50=0.7/0.9 nM) with ATP non-competitive and oral activity. Trametinib activates autophagy and induces apoptosis.
ターゲット＆IC50	MEK2:0.92 nM (cell free), MEK1:1.8 nM (cell free)
In vitro	METHODS: Mouse intrahepatic cholangiocarcinoma cells SB1, LD-1 and human intrahepatic cholangiocarcinoma cells EGI-1 were treated with Trametinib (0-10,000 nM) for 48 h, and cell growth inhibition was detected by MTT. RESULTS: Trametinib dose-dependently inhibited the growth of SB1, LD-1 and EGI-1 cells with IC50 of 41.48 nM, 56.10 nM and 27.89 nM, respectively. [1] METHODS: Human colon cancer cells RKO were treated with Trametinib (200 nmol/L) for 30 h. The expression levels of target proteins were detected by Western Blot. RESULTS: Trametinib significantly reduced the levels of p-ERK and p-AKT. [2] METHODS: Human glioma cells U87 and U251 were incubated with Trametinib (50 nM) for 6-72 h. Apoptosis was detected by Flow Cytometry. RESULTS: Trametinib induced a significant increase in apoptosis in U87 and U251 cells, and Trametinib induced late apoptosis but not early apoptosis in glioma cells. [3]
In vivo	METHODS: To detect anti-tumor activity in vivo, Trametinib (0.3-1 mg/kg) was orally administered to BALB/c-nu/nu mice bearing human colorectal cancer tumors HT-29 and COLO205 once daily for fourteen days. RESULTS: Trametinib treatment significantly inhibited the growth of human colorectal cancer tumors, indicating antitumor activity in vivo. [4] METHODS: To assay antitumor activity in vivo, Trametinib (5 mg/kg) was injected intraperitoneally three times a week for fourteen days into NSG mice bearing human B-lymphoblastic leukemia tumors KOPN8 and COLO205. RESULTS: Trametinib monotherapy delayed the progression of leukemia, but was not sufficient to prevent leukemia growth. [5]
キナーゼ試験	A Raf-MEK-ERK cascade kinase assay was carried out as previously described. Briefly, nonphosphorylated myelin basic protein (MBP) was coated onto an ELISA plate, and the active form of B-Raf/c-Raf was mixed with unphosphorylated MEK1/MEK2 and ERK2 in 10 μM ATP and 12.5 mM MgCl2 containing MOPS buffer in the presence of various concentrations of JTP-74057. The phosphorylation of MBP was detected by the anti-phosphoMBP antibody. Kinase inhibitory activities against a total of 99 kinases were tested by kinase profiler at 10 μM ATP [1].
細胞研究	These cells were maintained in media recommended by the providers. Exponentially growing cells were precultured in 96-well tissue culture plates for 24 h and then exposed to JTP-74057. Cell growth was determined by an in vitro toxicology assay kit, sulforhodamine B based. For combination studies, two compounds were simultaneously added to the HT-29 cells and incubated for 72 h. In the presence of various concentrations of compound A, the 50% inhibitory concentration (IC50) values of compound B were determined. Then, the fixed concentration of compound A versus the IC50 value of compound B was plotted. Conversely, the IC50 values of compound A were determined in the presence of various concentrations of compound B and plotted [1].
動物実験	Female BALB/c-nu/nu mice were used. On day 0, HT-29 cells or COLO205 cells suspended in ice-cold HBSS (-) were inoculated subcutaneously into the right flank of the mice at 5x10^6 cells/100 μl/site or 1x10^6 cells/100 μl/site, respectively. The acetic acid-solvated form of JTP-74057 was dissolved in 10% Cremophor EL-10% PEG400 and was administered orally once daily for 14 days from the day when the mean tumor volume reached 100 mm^3. The tumor length [L (mm)] and width [W (mm)] were measured using a micro gauge twice a week after the commencement of dosing, and the tumor volume was calculated using the following formula: tumor volume (mm^3) = L x W x W/2. All procedures relating to the use of animals in this study were reviewed and approved by the Institutional Animal Care and Use Committee of Japan Tobacco [1].

別名	GSK1120212, JTP-74057
分子量	615.39
分子式	C26H23FIN5O4
CAS No.	871700-17-3

保存条件

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度情報

DMSO: 7.86 mg/mL (12.77 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

参考文献

1. Wabitsch S, et al. Anti-PD-1 in Combination With Trametinib Suppresses Tumor Growth and Improves Survival of Intrahepatic Cholangiocarcinoma in Mice. Cell Mol Gastroenterol Hepatol. 2021;12(3):1166-1178. 2. Jing J, et al. Comprehensive predictive biomarker analysis for MEK inhibitor GSK112021Mol Cancer Ther. 2012 Mar;11(3):720-9. 3. Gao M, et al. Trametinib Inhibits the Growth and Aerobic Glycolysis of Glioma Cells by Targeting the PKM2/c-Myc Axis. Front Pharmacol. 2021 Oct 21;12:760055. 4. Yamaguchi T, et al. Antitumor activities of JTP-74057 (GSK1120212), a novel MEK1/2 inhibitor, on colorectal cancer cell lines in vitro and in vivo. Int J Oncol. 2011 Jul;39(1):23-31. 5. Kerstjens M, et al. Trametinib inhibits RAS-mutant MLL-rearranged acute lymphoblastic leukemia at specific niche sites and reduces ERK phosphorylation in vivo. Haematologica. 2018 Apr;103(4):e147-e150. 6. Wang X, Wu F, Wang H, et al. PDCD6 cooperates with C-Raf to facilitate colorectal cancer progression via Raf/MEK/ERK activation[J]. Journal of Experimental & Clinical Cancer Research. 2020, 39(1): 1-15.

引用文献

1. Jiang Z, Cheng L, Wu Z, et al. Transforming primary human hepatocytes into hepatocellular carcinoma with genetically defined factors. EMBO reports. 2022: e54275 2. Wang X, Wu F, Wang H, et al. PDCD6 cooperates with C-Raf to facilitate colorectal cancer progression via Raf/MEK/ERK activation. Journal of Experimental & Clinical Cancer Research. 2020, 39(1): 1-15 3. Sun C Y, Li Y Z, Cao D, et al. Rapamycin and trametinib: a rational combination for treatment of NSCLC. International Journal of Biological Sciences. 2021, 17(12): 3211-3223. 4. Lü Z, Li X, Li K, et al. Nitazoxanide and related thiazolides induce cell death in cancer cells by targeting the 20S proteasome with novel binding modes. Biochemical Pharmacology. 2022: 114913. 5. Klein C, Roussel G, Brun S, et al. 5-HIAA induces neprilysin to ameliorate pathophysiology and symptoms in a mouse model for Alzheimer’s disease. Acta Neuropathologica Communications. 2018 Dec 11;6(1):136 6. KieΔling M K, Nicolay J P, Schlör T, et al. NRAS mutations in cutaneous T cell lymphoma (CTCL) sensitize tumors towards treatment with the multikinase inhibitor Sorafenib. Oncotarget. 2017 Jul 11;8(28):45687-45697. 7. Meng Y, Lv T, Zhang J, et al.Temporospatial inhibition of Erk signaling is required for lymphatic valve formation.Signal Transduction and Targeted Therapy.2023, 8(1): 342. 8. Dong W, Lin M, Zhang R, et al.D-mannose targets PD-1 to lysosomal degradation and enhances T cell-mediated anti-tumor immunity.Cancer Letters.2024: 216883.

投与量変換

You can also refer to dose conversion for different animals. 詳細

In vivo投与量計算 (透明溶液)

ステップ1: 以下の情報を入力してください

投与量

mg/kg

動物の平均体重

動物あたりの投与量

動物数

溶媒の組成を入力してください

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

計算するリセット

計算結果:

作業濃度: mg/ml;

DMSO溶液の作成方法: mg あらかじめ溶解した薬剤 μL DMSO (マスター溶液の濃度 mg/mL)，濃度がそのバッチの薬剤のDMSO溶解度を超える場合は、まずご連絡ください。

生体内薬剤の調合法：取る μL DMSO マスター溶液、次に追加 μL PEG300，確実に混ぜてから加える μL Tween 80，確実に混ぜてから加える μL ddH₂O, 確実に混ぜる

お問合せ内容:

必ず順番通りに溶媒を加えてください。ボルテックスミキサーや超音波、湯煎することで溶解しやすくなります

計算器

モル濃度計算機

希釈計算機

再構成計算

分子量計算機

質量

濃度

体積

分子量

モル度計算機では以下の計算が可能です

既知の体積と濃度の溶液を調製するために必要な化合物の質量
質量が既知の化合物を目的の濃度まで溶解させるのに必要な溶液の量
特定の体積の中に既知の質量の化合物を入れて得られる溶液の濃度

参考例

モル濃度計算機を使用したモル濃度計算の例
化合物の分子量が197.13g/molである場合、10mlの水に10mMのストック溶液を作るのに必要な化合物の質量はどれくらいですか？
［分子量（MW）］の欄に［197.13］と入力してください
[濃度]ボックスに10と入力し、正しい単位（millimolar）を選択します
[容量]ボックスに10と入力し、正しい単位（milliliter）を選択します
計算を押します
答えの19.713mgが質量欄に表示されます

濃度 (開始)

体積 (開始)

濃度 (終了)

体積 (終了)

溶液を作るのに必要な希釈率の計算

溶液の調製に必要な希釈率の算出
希釈計算機は、既知の濃度の原液をどのように希釈するかを計算することができる便利なツールです。V1を計算するためにC1、C2＆V2を入力します。

参考例

Tocrisの希釈計算器を用いた希釈計算の一例
50μMの溶液を20ml作るためには、10mMの原液を何ml必要ですか？
C1V1=C2V2という式を用いて、C1=10mM、C2=50μM、V2=20ml、V1を未知数とします。
濃度（開始）ボックスに10を入力し正しい単位(millimolar)を選択してください
濃度（終了）ボックスに50を入力し正しい単位(millimolar)を選択してください
体積（終了）ボックスに20を入力し正しい単位(millimolar)を選択してください
計算を押します
100 microliter (0.1 ml) という答えが体積（開始）ボックスに表示されます。

分子式

分子量 g/mol

化合物の化学式を入力して、そのモル質量や元素組成を計算します

Tヒント：化学式は大文字と小文字を区別します。: C10H16N2O2 c10h16n2o2

化合物のモル質量（分子量）を計算する手順:
化学物質のモル質量を計算するには、その化学式を入力し、「計算」をクリックしてください。.
分子質量、分子量、モル質量、モル重量の定義:
分子質量（分子量）とは、物質の1分子の質量であり、統一された原子質量単位（u）で表されます。(1uは炭素12の1原子の質量の1/12に等しい）
モル質量（molar weight）とは、ある物質の1モルの質量のことで、単位はg/molです。

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技術サポート

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Trametinib 871700-17-3 Apoptosis Autophagy MAPK MEK inhibit MAP2K Inhibitor GSK1120212 orally type MAPKK collageninduced arthritis AIA GSK 1120212 JTP74057 Mitogen-activated protein kinase kinase GSK-1120212 JTP-74057 Adjuvant-induced JTP 74057 CIA inhibitor

本ウェブサイトに掲載されている製品は全て研究用試薬です。研究目的以外の用途にはご使用できません。

Trametinib

保存条件

溶解度情報

参考文献

引用文献

関連化合物ライブラリー

関連製品

投与量変換

In vivo投与量計算 (透明溶液)

計算器

モル度計算機では以下の計算が可能です

溶液を作るのに必要な希釈率の計算

バイアルを再構成するのに必要な溶媒の量を計算する.

化合物の化学式を入力して、そのモル質量や元素組成を計算します

技術サポート

Keywords