首页工具

登录

购物车

Tazemetostat

产品编号 T1788 CAS 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。

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。

Tazemetostat, CAS 1403254-99-8

规格	价格/CNY	货期
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 * 10 mM (in DMSO)	￥ 671	现货

大包装超大折扣，点击咨询

其他形式的 Tazemetostat:

选择批次

纯度: 99.82%

纯度: 99.72%

纯度: 99.48%

纯度: 99.38%

纯度: 98.73%

纯度: 98.66%

纯度: 98.24%

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

相关产品

拓展阅读

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
分子量	572.74
分子式	C34H44N4O4
CAS No.	1403254-99-8

存储

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

溶解度

DMSO: 33 mg/mL(57.6 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

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	1.746 mL	8.73 mL	17.4599 mL	43.6498 mL
	5 mM	0.3492 mL	1.746 mL	3.492 mL	8.73 mL
	10 mM	0.1746 mL	0.873 mL	1.746 mL	4.365 mL
	20 mM	0.0873 mL	0.4365 mL	0.873 mL	2.1825 mL
	50 mM	0.0349 mL	0.1746 mL	0.3492 mL	0.873 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

质量

=

浓度

X

容积

X

分子量

浓度 (起始)

X

容积 (起始)

=

浓度 (终)

X

容积 (终)

溶液体积

=

质量

/

配液浓度

参考文献

1. Kawano S, et al. Preclinical Evidence of Anti-Tumor Activity Induced by EZH2 Inhibition in Human Models of Synovial Sarcoma. PLoS One. 2016 Jul 8;11(7):e0158888. 2. Knutson SK, et al. Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZHProc Natl Acad Sci U S A. 2013 May 7;110(19):7922-7. 3. Luo Y, et al. Inhibition of EZH2 (Enhancer of Zeste Homolog 2) Attenuates Neuroinflammation via H3k27me3/SOCS3/TRAF6/NF-κB (Trimethylation of Histone 3 Lysine 27/Suppressor of Cytokine Signaling 3/Tumor Necrosis Factor Receptor Family 6/Nuclear Factor-κB) in a Rat Model of Subarachnoid Hemorrhage. Stroke. 2020 Nov;51(11):3320-3331. 5. Cao Shangtao, Shengyong Yu, Dongwei Li, Jing Ye, Xuejie Yang, Chen Li, Xiaoshan Wang et al. Chromatin accessibility dynamics during chemical induction of pluripotency[J]. Cell stem cell. 2018 Apr 22(4): 529-542. e5.

文献引用

1. Song P, Duan J L, Ding J, et al.Cellular senescence primes liver fibrosis regression through Notch‐EZH2.MedComm.2023, 4(5): e346. 2. Zhang Q, Chen X, Cao J, et al.Discovery of a Novel Covalent EZH2 Inhibitor Based on Tazemetostat Scaffold for the Treatment of Ovarian Cancer.Journal of Medicinal Chemistry.2023 3. Yang Y, Xiao L, Xue Y, et al.ZBTB7A regulates primed‐to‐naïve transition of pluripotent stem cells via recognition of the PNT‐associated sequence by Zinc Fingers 1–2 and recognition of γ‐globin− 200 gene element by Zinc Fingers 1–4.The FEBS Journal.2023 4. Gu T, Xu C, Meng X, et al.Sevoflurane Preconditioning Alleviates Posttraumatic Stress Disorder—Induced Apoptosis in the Hippocampus via the EZH2-Regulated Akt/mTOR Axis and Improves Synaptic Plasticity.Journal of Molecular Neuroscience.2023: 1-12. 5. Ghildiyal R, Sawant M, Renganathan A, et al. Loss of Long Noncoding RNA NXTAR in Prostate Cancer Augments Androgen Receptor Expression and Enzalutamide ResistanceTumor Suppressor lncRNA NXTAR Inhibits AR/AR-V7 Expression. Cancer Research. 2022, 82(1): 155-168 6. Ghildiyal R, Sawant M, Renganathan A, et al. Loss of long non-coding RNA NXTAR in prostate cancer augments androgen receptor expression and enzalutamide resistance. Cancer Research. 2021 7. Ghildiyal R, Sawant M, Renganathan A, et al. Loss of Long Noncoding RNA NXTAR in Prostate Cancer Augments Androgen Receptor Expression and Enzalutamide Resistance. Cancer Research. 2022, 82(1): 155-168 8. Luo Y, Fang Y, Kang R, et al. Inhibition of EZH2 (Enhancer of Zeste Homolog 2) Attenuates Neuroinflammation via H3k27me3/SOCS3/TRAF6/NF-κB (Trimethylation of Histone 3 Lysine 27/Suppressor of Cytokine Signaling 3/Tumor Necrosis Factor Receptor Family 6/Nuclear Factor-κB) in a Rat Model of Subarachnoid Hemorrhage. Stroke. 2020: STROKEAHA. 120.029951 9. Zhang L, Qu J, Qi Y, et al. EZH2 engages TGFβ signaling to promote breast cancer bone metastasis via integrin β1-FAK activation. Nature Communications. 2022, 13(1): 1-16 10. Cao Shangtao, Shengyong Yu, Dongwei Li, Jing Ye, Xuejie Yang, Chen Li, Xiaoshan Wang et al. Chromatin accessibility dynamics during chemical induction of pluripotency. Cell Stem Cell. 2018, 22(4): 529-542. e5

11. Yu S, Zhou C, Cao S, et al. BMP4 resets mouse epiblast stem cells to naive pluripotency through ZBTB7A/B-mediated chromatin remodelling. Nature cell biology. 2020: 1-12. 12. Yu S, Zhou C, He J, et al. BMP4 drives primed to naïve transition through PGC-like state. Nature Communications. 2022, 13(1): 1-15

下拉查看更多收起

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

%DMSO+

%

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

Tazemetostat 1403254-99-8 Chromatin/Epigenetic Histone Methyltransferase epigenetic inhibit EPZ-6438 Inhibitor E 7438 EPZ 6438 E7438 EZH1 cancer E-7438 EZH2 PRC2 EPZ6438 inhibitor

我们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。

沪公网安备 31010602006700号

陶术

生物

TargetMol^®中国区唯一合作伙伴

点击进入陶术生物官网

联系我们

电话：

400-820-0310

邮箱：

service@tsbiochem.com

QQ：

2881945090（终端用户）

2885109491（经销商）

经销：

终端：

地址：

上海市静安区江场三路238号8楼

Tazemetostat

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords