Tazemetostat(Synonyms: EPZ-6438; E-7438)

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Tazemetostat (Synonyms: EPZ-6438; E-7438) 纯度: 99.93%

Tazemetostat (EPZ-6438) 是一种有效，选择性，口服的 EZH2 抑制剂。Tazemetostat (EPZ-6438) 抑制含有 PRC2 复合体的野生型 EZH2 的活性， Ki 值为 2.5±0.5 nM。Tazemetostat (EPZ-6438) 抑制 EZH2，在肽测定和核小体测定中 IC50 分别为 11 和 16 nM。Tazemetostat (EPZ-6438) 抑制大鼠 EZH2，IC50 为 4 nM。Tazemetostat (EPZ-6438) 还抑制 EZH1，IC50 为 392 nM。

Tazemetostat(Synonyms: EPZ-6438; E-7438)

Tazemetostat Chemical Structure

CAS No. : 1403254-99-8

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10 mM * 1 mL in DMSO ￥756 In-stock
5 mg ￥600 In-stock
10 mg ￥900 In-stock
50 mg ￥2100 In-stock
100 mg ￥3500 In-stock
200 mg ￥6100 In-stock
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生物活性

Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat (EPZ-6438) inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat (EPZ-6438) inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat (EPZ-6438) inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat (EPZ-6438) also inhibits EZH1 with an IC50 of 392 nM[1].

IC50 & Target[1]

EZH2

11 nM (IC50, in peptide assay)

EZH2

16 nM (IC50, in nucleosome assay)

Rat EZH2

4 nM (IC50)

EZH1

392 nM (IC50)

EZH2 WT

2.5 nM (Ki)

体外研究
(In Vitro)

Tazemetostat (EPZ-6438) inhibits multi wild-type and mutant lymphoma cell lines proliferation with IC50s of 0.49 nM-7.6 μM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: Wild-type and mutant lymphoma cell lines: DOHH-2 cell (EZH2 wild-type), Farage cell (EZH2 wild-type), OCI-LY19 cell (EZH2 wild-type), Toledo cell (EZH2 wild-type), KARPAS-422 (EZH2 Y646N), Pfeiffer (EZH2 A682G), RL cell line (EZH2 Y646N), SU-DHL-10 (EZH2 Y646F), SU-DHL-6 (EZH2 Y646N), WSU-DLCL2 (EZH2 Y646F)
Concentration: 0.49 nM-7.6 μM
Incubation Time: 11 days
Result: Inhibited DOHH-2 cell (EZH2 wild-type; IC50=1.7 μM), Farage cell (EZH2 wild-type; IC50=99 nM), OCI-LY19 cell (EZH2 wild-type; IC50=6.2 μM), Toledo cell (EZH2 wild-type; IC50=7.6 μM), KARPAS-422 (EZH2 Y646N; IC50=1.8 nM), Pfeiffer (EZH2 A682G; IC50=0.49 nM), RL cell line (EZH2 Y646N; IC50=5.8 μM), SU-DHL-10 (EZH2 Y646F; IC50=5.8 nM), SU-DHL-6 (EZH2 Y646N; IC50=4.7 nM), WSU-DLCL2 (EZH2 Y646F; IC50=8.6 nM) proliferation.

体内研究
(In Vivo)

Tazemetostat (EPZ-6438; 250 or 500 mg/kg twice daily for 21-28 days) practically eliminates the fast-growing G401 tumors[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SCID mice bearing s.c. G401 xenografts[1]
Dosage: 125 mg/kg, 250 mg/kg, 500 mg/kg
Administration: Oral; twice daily; 28 days
Result: Practically eliminated the fast-growing G401 tumors at 250 or 500 mg/kg.

Clinical Trial

分子量

572.74

Formula

C34H44N4O4
CAS 号

1403254-99-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (218.25 mM; ultrasonic and warming and heat to 60°C)

0.1 M HCL : 14.29 mg/mL (24.95 mM; ultrasonic and adjust pH to 5 with HCl)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7460 mL 8.7300 mL 17.4599 mL
5 mM 0.3492 mL 1.7460 mL 3.4920 mL
10 mM 0.1746 mL 0.8730 mL 1.7460 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 0.5% CMC-Na    0.1% Tween-80

    Solubility: 50 mg/mL (87.30 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂： 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (4.36 mM); Clear solution

  • 3.

    请依序添加每种溶剂： 5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.36 mM); Clear solution

  • 4.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.63 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.63 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 5.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.63 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.63 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 6.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.63 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.63 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Knutson SK, et al. Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferaseEZH2. Proc Natl Acad Sci U S A. 2013 May 7;110(19):7922-7.

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