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Trametinib

产品编号 T2125 CAS 871700-17-3

别名: GSK1120212, 曲美替尼, JTP-74057

Trametinib (GSK1120212) 是一种 MEK 抑制剂，抑制 MEK1 和 MEK2 (IC50=0.7/0.9 nM)，具有 ATP 非竞争性和口服活性。Trametinib 可以激活自噬，诱导凋亡。

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Trametinib Chemical Structure

Trametinib, CAS 871700-17-3

规格	价格/CNY		货期	数量
10 mg	￥ 282		现货
25 mg	￥ 452		现货
50 mg	￥ 654		现货
100 mg	￥ 1,050		现货
500 mg	￥ 2,537		现货
1 mL * 10 mM (in DMSO)	￥ 320		现货

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其他形式的 Trametinib:

Trametinib (DMSO solvate)
现货

选择批次

纯度: 99.88%

纯度: 99.88%

纯度: 99.88%

纯度: 99.72%

纯度: 99.71%

纯度: 99.39%

纯度: 98%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	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.
靶点活性	MEK2:0.92 nM (cell free), MEK1:1.8 nM (cell free)
体外活性	方法：小鼠肝内胆管癌细胞 SB1、LD-1 和人肝内胆管癌细胞 EGI-1 用 Trametinib (0-10000 nM) 处理 48 h，使用 MTT 方法检测细胞生长抑制情况。结果：Trametinib 剂量依赖抑制 SB1、LD-1 和 EGI-1 细胞生长，IC50 分别为 41.48 nM、56.10 nM 和 27.89 nM。[1] 方法：人结肠癌细胞 RKO 用 Trametinib (200 nmol/L) 处理 30 h，使用 Western Blot 方法检测靶点蛋白表达水平。结果：Trametinib 显著降低 p-ERK 和 p-AKT 水平。[2] 方法：人胶质瘤细胞 U87 和 U251 用 Trametinib (50 nM) 孵育 6-72 h，使用 Flow Cytometry 方法检测细胞凋亡情况。结果：Trametinib 诱导 U87 和 U251 细胞的凋亡率明显增加。Trametinib 可以诱导神经胶质瘤细胞的晚期凋亡，而不会发生早期凋亡。[3]
体内活性	方法：为检测体内抗肿瘤活性，将 Trametinib (0.3-1 mg/kg) 口服给药给携带人结直肠癌肿瘤 HT-29 和 COLO205 的 BALB/c-nu/nu 小鼠，每天一次，持续十四天。结果：Trametinib 治疗显著抑制人结直肠癌肿瘤的生长，表明在体内具有抗肿瘤活性。[4] 方法：为检测体内抗肿瘤活性，将 Trametinib (5 mg/kg) 腹腔注射给携带人B淋巴细胞白血病肿瘤 KOPN8 和 COLO205 的 NSG 小鼠，每周三次，持续十四天。结果：Trametinib 单药治疗延缓了白血病的进展，但不足以防止白血病的生长。[5]
激酶实验	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].
细胞实验	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].
动物实验	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].

别名	GSK1120212, 曲美替尼, JTP-74057
化合物与蛋白结合的复合物	Crystal Structure of KSR2:MEK1 in complex with AMP-PNP, and allosteric MEK inhibitor Trametinib
分子量	615.39
分子式	C26H23FIN5O4
CAS No.	871700-17-3

存储

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

溶解度

DMSO: 7.86 mg/mL (12.77 mM)

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

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.625 mL	8.1249 mL	16.2499 mL	40.6246 mL
	5 mM	0.325 mL	1.625 mL	3.25 mL	8.1249 mL
	10 mM	0.1625 mL	0.8125 mL	1.625 mL	4.0625 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

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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.

文献引用

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.

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相关化合物库

该产品包含在如下化合物库中：

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剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

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每只动物体重

g

给药体积

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动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

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% Tween 80+

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计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

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

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