JQEZ5|cas:1913252-04-6|西域试剂

JQEZ5,98.08%

产品编号：Bellancom-100846| CAS NO：1913252-04-6| 分子式：C₃₀H₃₈N₈O₂| 分子量：542.68

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货号	价格	库存与货期
Bellancom-100846	￥1100.00	杭州北京（现货）
Bellancom-100846	￥1600.00	杭州北京（现货）
Bellancom-100846	￥6000.00	杭州北京（现货）
Bellancom-100846	￥10500.00	杭州北京（现货）

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JQEZ5

产品介绍

JQEZ5 是一种有效的选择性的 EZH2 赖氨酸甲基转移酶抑制剂。JQEZ5 以 SAM 竞争性方式抑制 PRC2 的酶功能，IC₅₀ 为 80 nM。JQEZ5 具有抗肿瘤作用。

生物活性

JQEZ5 is a potent and selective EZH2 lysine methyltransferase inhibitor. JQEZ5 SAM-competitively inhibits polycomb repressive complex 2 (PRC2) with an IC₅₀ of 80 nM. JQEZ5 has anti-tumor effects.

体外研究

JQEZ5 inhibits enzymatic functionality of PRC2 with a biochemical IC50 of 80nM. JQEZ5 exhibits S-adenosyl methionine (SAM)-competitive inhibition of PRC2.
H661 cells treated with increasing concentrations of JQEZ5 demonstrate acutely reduced levels of H3K27me3 without affecting H3K27 mono- or di-methylation. JQEZ5 suppresses the proliferation of EZH2-overexpressing H661 and H522 cells after treatment for 4 days without affecting the proliferation of cell lines that were deemed insensitive to EZH2 knockdown.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

JQEZ5 (75 mg/kg; intraperitoneal injection; daily; for 3 weeks) treatment exhibits rapid and pronounced tumor regression over the three week treatment course. And H3K27me3 levels are largely reduced with treatment further confirming the on-target effect of JQEZ5 in mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (46.07 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8427 mL	9.2135 mL	18.4271 mL
5 mM	0.3685 mL	1.8427 mL	3.6854 mL
10 mM	0.1843 mL	0.9214 mL	1.8427 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： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.61 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.61 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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