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Trametinib

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产品编号 T2125Cas号 871700-17-3
别名 曲美替尼, JTP-74057, GSK1120212

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。

Trametinib

Trametinib

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纯度: 99.88%
产品编号 T2125 别名 曲美替尼, JTP-74057, GSK1120212Cas号 871700-17-3

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。

规格价格库存数量
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 x 10 mM (in DMSO)¥ 320现货
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产品介绍

生物活性
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
MEK1:1.8 nM (cell free), MEK2:0.92 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].
别名曲美替尼, JTP-74057, GSK1120212
化学信息
分子量615.39
分子式C26H23FIN5O4
CAS No.871700-17-3
SmilesN(C1=C2C(N(C(=O)N(C2=O)C3CC3)C4=CC(NC(C)=O)=CC=C4)=C(C)C(=O)N1C)C5=C(F)C=C(I)C=C5
密度1.743 g/cm3
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2.1 mg/mL (3.41 mM), In vivo: Suspension. Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
DMSO: 7.86 mg/mL (12.77 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
溶液配制表
DMSO
1mg5mg10mg50mg
5 mM0.3250 mL1.6250 mL3.2500 mL16.2499 mL
10 mM0.1625 mL0.8125 mL1.6250 mL8.1249 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

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:
TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent 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 μLDMSOTargetMol | reagent ( 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 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

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