购物车
  • 全部删除
  • TargetMol
    您的购物车当前为空

Tazemetostat

产品编号 T1788Cas号 1403254-99-8
别名 E-7438, EPZ6438

Tazemetostat (EPZ6438) 是一种组蛋白甲基转移酶 EZH2 抑制剂 (IC50=11 nM),具有口服活性、选择性和 SAM 竞争性。Tazemetostat 具有抗肿瘤活性,可以用于治疗上皮样肉瘤/滤泡性淋巴瘤。

Tazemetostat

Tazemetostat

纯度: ≥95%
产品编号 T1788 别名 E-7438, EPZ6438Cas号 1403254-99-8

Tazemetostat (EPZ6438) 是一种组蛋白甲基转移酶 EZH2 抑制剂 (IC50=11 nM),具有口服活性、选择性和 SAM 竞争性。Tazemetostat 具有抗肿瘤活性,可以用于治疗上皮样肉瘤/滤泡性淋巴瘤。

规格价格库存数量
5 mg¥ 537现货
10 mg¥ 822现货
50 mg¥ 1,962现货
100 mg¥ 3,292现货
200 mg¥ 4,450现货
1 mL x 10 mM (in DMSO)¥ 671现货
大包装 & 定制
加入购物车
实验操作小课堂
查看更多

"Tazemetostat"的相关化合物库

选择批次:
纯度:≥95%
联系我们获取更多批次信息
TargetMol 的所有产品仅用作科学研究或药证申报,不能被用于人体,我们不向个人提供产品和服务。请您遵守承诺用途,不得违反法律法规规定用于任何其他用途。

产品介绍

生物活性
产品描述
Tazemetostat (EPZ6438) is a histone methyltransferase EZH2 inhibitor (IC50=11 nM) that is orally active, selective, and SAM-competitive. Tazemetostat exhibits antitumor activity and may be used for the treatment of epithelioid sarcoma/follicular lymphoma.
靶点活性
EZH2:2.5 nM(Ki)
体外活性
方法:滑膜肉瘤细胞 Fuji 和 HS-SY-II 用 Tazemetostat (0.039-20 µmol/L) 处理 14 天,使用 CellTiter-Glo Luminescent Cell Viability Assay 检测细胞活力。
结果:Tazemetostat 处理 Fuji 和 HS-SY-II 细胞增殖的浓度依赖性降低,IC50 值分别为 0.15 µmol/L 和 0.52 µmol/L。[1]
方法:人肾癌细胞 G401 和人恶性胚胎横纹肌瘤细胞 RD 用 Tazemetostat (0.006-1100 nM) 处理 4 天,使用 Western Blot 方法检测靶点蛋白表达水平。
结果:Tazemetostat 处理导致整体 H3K27Me3 水平的浓度依赖性降低。[2]
体内活性
方法:为检测体内抗肿瘤活性,将 Tazemetostat (125-500 mg/kg,0.5% NaCMC plus 0.1% Tween 80 in water) 口服给药给携带人肾癌肿瘤 G401 的 SCID 小鼠,每天两次,持续二十八天。
结果:Tazemetostat 导致 SMARCB1突变型 MRT 异种移植物完全和持续消退。[1]
方法:为研究在蛛网膜下腔出血 (SAH) 诱导的神经炎症中的作用,将 Tazemetostat (1-9 mg/kg) 腹腔注射给血管内穿孔法诱导蛛网膜下腔出血的大鼠模型。
结果:Tazemetostat 对 EZH2 的抑制通过 H3K27me3/SOCS3/TRAF6/NF-κB 信号通路减轻了大鼠 SAH 后的神经炎症。[3]
激酶实验
Biochemical Methods: EPZ-6438 is incubated for 30 min with 40 μL per well of 5 nM PRC2 (final assay concentration in 50 μL is 4 nM ) in 1X assay buffer (20 mM Bicine [pH 7.6], 0.002% Tween-20, 0.005% Bovine Skin Gelatin and 0.5 mM DTT). 10 μL per well of substrate mix comprising assay buffer 3 H-SAM, unlabeled SAM, and peptide representing histone H3 residues 21-44 containing C-terminal biotin (appended to a C-terminal amide-capped lysine) are added to initiate the reaction (both substrates are present in the final reaction mixture at their respective Km values, an assay format referred to as ‘‘balanced conditions''. The final concentrations of substrates and methylation state of the substrate peptide are indicated for each enzyme Reactions are incubated for 90 min at room temperature and quenched with 10 μL per well of 600 μM unlabeled SAM, Then transferred to a 384-well flashplate and washed after 30 min.
细胞实验
For the adherent cell line proliferation assays, plating densities for each cell line are determined based on growth curves (measured by ATP content) and density over a 7-d time course. On the day before compound treatment, cells are plated in either 96-well plates in triplicate (for the day 0–7 time course) or 6-well plates (for replating on day 7 for the remainder of the time course). On day 0, cells are either untreated, DMSO-treated, or treated with EPZ-6438 starting at 10 μM and decreasing in either threefold or fourfold dilutions. Plates are read on day 0, day 4, and day 7 using Cell Titer Glo, with compound/media being replenished on day 4. On day 7, the six-well plates are trypsinized, centrifuged, and resuspended in fresh media for counting by Vi-Cell. Cells from each treatment are replated at the original density in 96-well plates in triplicate. Cells are allowed to adhere to the plate overnight, and cells are treated as on day 0. On days 7, 11, and 14, plates are read using Cell Titer Glo, with compound/media being replenished on day 11. Averages of triplicates are used to plot proliferation over the time course, and calculate IC50 values. For cell cycle and apoptosis, G401 and RD cells are plated in 15-cm dishes in duplicate at a density of 1 × 106 cells per plate. Cells are incubated with EPZ-6438 at 1 μM, in a total of 25 mL, over a course of 14 d, with cells being split back to original plating density on day 4, 7, and 11. Cell cycle analysis and TUNEL assay are performed using a Guava flow cytometer, following the manufacturer's protocol.(Only for Reference)
别名E-7438, EPZ6438
化学信息
分子量572.74
分子式C34H44N4O4
CAS No.1403254-99-8
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: 3.3 mg/mL (5.76 mM), 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: 29.2 mg/mL (50.98 mM), Sonication and heating are recommended.
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
溶液配制表
10% DMSO+40% PEG300+5% Tween 80+45% Saline/DMSO
1mg5mg10mg50mg
1 mM1.7460 mL8.7300 mL17.4599 mL87.2996 mL
5 mM0.3492 mL1.7460 mL3.4920 mL17.4599 mL
DMSO
1mg5mg10mg50mg
10 mM0.1746 mL0.8730 mL1.7460 mL8.7300 mL
20 mM0.0873 mL0.4365 mL0.8730 mL4.3650 mL
50 mM0.0349 mL0.1746 mL0.3492 mL1.7460 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

剂量转换

对于不同动物的给药剂量换算,您也可以参考 更多

关键词

Related Tags: buy Tazemetostat | purchase Tazemetostat | Tazemetostat cost | order Tazemetostat | Tazemetostat chemical structure | Tazemetostat in vivo | Tazemetostat in vitro | Tazemetostat formula | Tazemetostat molecular weight