化合物 EPZ6438|T1788

Tazemetostat
1403254-99-8

￥537 5mg 起订

￥822 10mg 起订

￥1962 50mg 起订

上海更新日期：2024-09-14

TargetMol中国（陶术生物）

VIP12年

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 化合物 EPZ6438

英文名称：: Tazemetostat

CAS号：: 1403254-99-8

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: ≥95%

产品类别：: 抑制剂

货号：: T1788

Product Introduction

Bioactivity

名称	Tazemetostat
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.
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)
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.
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]
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	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)
关键字	epigenetic \| inhibit \| Tazemetostat \| Histone Methyltransferase \| EPZ-6438 \| Inhibitor \| E 7438 \| EPZ 6438 \| E7438 \| EZH1 \| cancer \| EZH2 \| PRC2
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相关库	抑制剂库 \| 抗癌上市药物库 \| 抗癌活性化合物库 \| 经典已知活性库 \| 已知活性化合物库 \| 抗衰老化合物库 \| 高选择性抑制剂库 \| FDA 上市药物库 \| 抗癌临床化合物库 \| 抗癌药物库

E-7438|||EPZ6438|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子