Tazemetostat

カタログ番号 T1788 CAS 1403254-99-8

別名: E-7438, EPZ6438

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.

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Tazemetostat, CAS 1403254-99-8

パッケージサイズ	在庫状況	単価(税別)
サンプルについてお問い合わせ
5 mg	在庫あり	￥ 13,500
10 mg	在庫あり	￥ 18,500
50 mg	在庫あり	￥ 26,000
100 mg	在庫あり	￥ 40,500
200 mg	在庫あり	￥ 61,000
500 mg	在庫あり	￥ 114,000
1 mL * 10 mM (in DMSO)	在庫あり	￥ 17,000

バルクのお問い合わせ

バッチを選択

純度: 99.82%

COA DATASHEET SDS HNMR HPLC

純度: 99.72%

COA DATASHEET SDS HNMR HPLC

純度: 99.48%

COA DATASHEET SDS HPLC HNMR

純度: 99.38%

COA DATASHEET SDS HNMR HPLC

純度: 98.73%

COA DATASHEET SDS HPLC HNMR

純度: 98.66%

COA DATASHEET SDS HNMR HPLC

純度: 98.24%

COA DATASHEET SDS HNMR HPLC

純度: 98%

COA DATASHEET SDS HNMR

COA DATASHEET SDS

COA DATASHEET SDS HNMR

バッチの詳細情報はお問い合わせください

生物学的特性に関する説明

化学的特性

保存条件 & 溶解度情報

説明	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.
ターゲット＆IC50	EZH2:2.5 nM(Ki)
In vitro	METHODS: Synovial sarcoma cells Fuji and HS-SY-II were treated with Tazemetostat (0.039-20 µmol/L) for 14 days, and cell viability was measured using the CellTiter-Glo Luminescent Cell Viability Assay. RESULTS: Concentration-dependent reduction of cell proliferation was observed in Tazemetostat-treated Fuji and HS-SY-II cells, with IC50 values of 0.15 µmol/L and 0.52 µmol/L, respectively. [1] METHODS: Human renal cancer cells G401 and human malignant embryonic rhabdomyosarcoma cells RD were treated with Tazemetostat (0.006-1100 nM) for 4 days, and the expression levels of the target proteins were detected by Western Blot. RESULTS: Tazemetostat treatment resulted in a concentration-dependent decrease in overall H3K27Me3 levels. [2] Translated with DeepL.com (free version)
In vivo	METHODS: To assay antitumor activity in vivo, Tazemetostat (125-500 mg/kg, 0.5% NaCMC plus 0.1% Tween 80 in water) was administered orally to SCID mice harboring human renal carcinoma tumor G401 twice a day for twenty-eight days. RESULTS: Tazemetostat caused complete and sustained regression of SMARCB1 mutant MRT xenografts. [1] METHODS: To investigate the role in subarachnoid hemorrhage (SAH)-induced neuroinflammation, Tazemetostat (1-9 mg/kg) was administered intraperitoneally to a rat model of subarachnoid hemorrhage induced by endovascular perforation. RESULTS: Inhibition of EZH2 by Tazemetostat attenuated neuroinflammation after SAH in rats via the H3K27me3/SOCS3/TRAF6/NF-κB signaling pathway. [3]
キナーゼ試験	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.
細胞研究	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)

別名	E-7438, EPZ6438
分子量	572.74
分子式	C34H44N4O4
CAS No.	1403254-99-8

保存条件

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

溶解度情報

DMSO: 33 mg/mL(57.6 mM)

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

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

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.

引用文献

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

もっと見る隠し

投与量変換

You can also refer to dose conversion for different animals. 詳細

In vivo投与量計算 (透明溶液)

ステップ1: 以下の情報を入力してください

投与量

mg/kg

動物の平均体重

動物あたりの投与量

動物数

溶媒の組成を入力してください

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

計算するリセット

計算結果:

作業濃度: mg/ml;

DMSO溶液の作成方法: mg あらかじめ溶解した薬剤 μL DMSO (マスター溶液の濃度 mg/mL)，濃度がそのバッチの薬剤のDMSO溶解度を超える場合は、まずご連絡ください。

生体内薬剤の調合法：取る μL DMSO マスター溶液、次に追加 μL PEG300，確実に混ぜてから加える μL Tween 80，確実に混ぜてから加える μL ddH₂O, 確実に混ぜる

お問合せ内容:

必ず順番通りに溶媒を加えてください。ボルテックスミキサーや超音波、湯煎することで溶解しやすくなります

計算器

モル濃度計算機

希釈計算機

再構成計算

分子量計算機

質量

濃度

体積

分子量

モル度計算機では以下の計算が可能です

既知の体積と濃度の溶液を調製するために必要な化合物の質量
質量が既知の化合物を目的の濃度まで溶解させるのに必要な溶液の量
特定の体積の中に既知の質量の化合物を入れて得られる溶液の濃度

参考例

モル濃度計算機を使用したモル濃度計算の例
化合物の分子量が197.13g/molである場合、10mlの水に10mMのストック溶液を作るのに必要な化合物の質量はどれくらいですか？
［分子量（MW）］の欄に［197.13］と入力してください
[濃度]ボックスに10と入力し、正しい単位（millimolar）を選択します
[容量]ボックスに10と入力し、正しい単位（milliliter）を選択します
計算を押します
答えの19.713mgが質量欄に表示されます

濃度 (開始)

体積 (開始)

濃度 (終了)

体積 (終了)

溶液を作るのに必要な希釈率の計算

溶液の調製に必要な希釈率の算出
希釈計算機は、既知の濃度の原液をどのように希釈するかを計算することができる便利なツールです。V1を計算するためにC1、C2＆V2を入力します。

参考例

Tocrisの希釈計算器を用いた希釈計算の一例
50μMの溶液を20ml作るためには、10mMの原液を何ml必要ですか？
C1V1=C2V2という式を用いて、C1=10mM、C2=50μM、V2=20ml、V1を未知数とします。
濃度（開始）ボックスに10を入力し正しい単位(millimolar)を選択してください
濃度（終了）ボックスに50を入力し正しい単位(millimolar)を選択してください
体積（終了）ボックスに20を入力し正しい単位(millimolar)を選択してください
計算を押します
100 microliter (0.1 ml) という答えが体積（開始）ボックスに表示されます。

分子式

分子量 g/mol

化合物の化学式を入力して、そのモル質量や元素組成を計算します

Tヒント：化学式は大文字と小文字を区別します。: C10H16N2O2 c10h16n2o2

化合物のモル質量（分子量）を計算する手順:
化学物質のモル質量を計算するには、その化学式を入力し、「計算」をクリックしてください。.
分子質量、分子量、モル質量、モル重量の定義:
分子質量（分子量）とは、物質の1分子の質量であり、統一された原子質量単位（u）で表されます。(1uは炭素12の1原子の質量の1/12に等しい）
モル質量（molar weight）とは、ある物質の1モルの質量のことで、単位はg/molです。

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技術サポート

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

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

本ウェブサイトに掲載されている製品は全て研究用試薬です。研究目的以外の用途にはご使用できません。

Tazemetostat

保存条件

溶解度情報

参考文献

引用文献

関連化合物ライブラリー

関連製品

投与量変換

In vivo投与量計算 (透明溶液)

計算器

モル度計算機では以下の計算が可能です

溶液を作るのに必要な希釈率の計算

バイアルを再構成するのに必要な溶媒の量を計算する.

化合物の化学式を入力して、そのモル質量や元素組成を計算します

技術サポート

Keywords