首页 工具
登录
购物车
Trametinib

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

TargetMol的所有产品和服务仅用于科学研究,不能被用于人体,我们也不向个人提供产品和服务。
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
其他形式的 Trametinib:
产品目录号及名称: Trametinib (T2125)
点击图片重新获取验证码
选择批次  
纯度: 99.88%
纯度: 99.72%
纯度: 99.71%
纯度: 99.39%
纯度: 98%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
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

T2125_2

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: 21 mg/mL (34.1 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
20 mM 0.0812 mL 0.4062 mL 0.8125 mL 2.0312 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
=
X
X
X
=
X
=
/
g/mol

输入分子式,点击计算,可计算出产品的分子量。

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.
Calcium dobesilate OTS514 hydrochloride Adapalene Evocarpine DB1976 PD0166285 2-Thiocytidine CM-272

相关化合物库

该产品包含在如下化合物库中:
抗癌上市药物库 酪氨酸激酶分子库 高选择性抑制剂库 神经退行性疾病化合物库 抗癌临床化合物库 抗癌药物库 抗癌活性化合物库 临床前化合物库 FDA上市及药典收录分子库 含氟化合物库

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
mg/kg
每只动物体重
g
给药体积
μL
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
%
% Tween 80
% ddH2O
计算 重置

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

 

陶术
生物
TargetMol®中国区唯一合作伙伴
点击进入陶术生物官网陶术生物
联系我们
400-820-0310

上海市静安区江场三路238号8楼