EN4|cas:1197824-15-9|西域试剂

EN4,97.05%

产品编号：Bellancom-134761| CAS NO：1197824-15-9| 分子式：C₂₅H₂₄N₂O₄| 分子量：416.47

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货号	价格	库存与货期
Bellancom-134761	￥900.00	杭州北京（现货）
Bellancom-134761	￥1100.00	杭州北京（现货）
Bellancom-134761	￥2500.00	杭州北京（现货）
Bellancom-134761	￥3600.00	杭州北京（现货）
Bellancom-134761	￥5400.00	杭州北京（现货）

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EN4

产品介绍

EN4 是一种针对 MYC 的半胱氨酸 171 (C171) 的共价配体。EN4 对 c-MYC 的选择性高于 N-MYC 和 L-MYC。EN4 抑制 MYC 转录活性，下调 MYC 靶标，并具有抗肿瘤作用。

生物活性

EN4 is a covalent ligand that targets cysteine 171 (C171) of MYC. EN4 is selective for c-MYC over N-MYC and L-MYC. EN4 inhibits MYC transcriptional activity, downregulates MYC targets, and impairs tumorigenesis.

体外研究

EN4 (1-50 μM; for 72 hours) treatment significantly impaires 231MFP breast cancer cell proliferation in a dosedependent manner, with >90% inhibition of proliferation at 50 μM.
EN4 (50 μM; for 60 hours) treatment significantly decreases the protein levels of representative MYC-regulated target genes, including CDK2 and CDC25A. EN4 treatment also substantially reduces MYC levels.
EN4 shows the strongest inhibition of both MYC/MAX binding to its DNA consensus sequence in vitro as well as MYC transcriptional activity in cells. EN4 inhibited MYC/MAX binding to the E-box response element DNA consensus sequence in a dose-responsive manner with an IC50 value of 6.7 μM. EN4 also inhibits MYC luciferase reporter activity in a dose-responsive manner with an IC50 value of 2.8 μM.
EN4 (50 μM; for 2 hours) treatment significantly reduced MYC thermal stability in 231MFP breast cancer cells.

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

Cell Proliferation Assay

Cell Line:	231MFP breast cancer cells
Concentration:	1 μM, 10 μM, 50 μM
Incubation Time:	72 hours
Result:	Significantly impaired 231MFP breast cancer cell proliferation in a dose-dependent manner.

Western Blot Analysis

Cell Line:	231MFP breast cancer cells
Concentration:	50 μM
Incubation Time:	60 hours
Result:	The protein levels of CDK2 and CDC25A were significantly lowered.

体内研究
(In Vivo)

EN4 (50 mg/kg; intraperitoneal injection; daily; for 3 weeks) treatment significantly attenuated tumor growth in 231MFP breast tumor xenograft mice.

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

Animal Model:	SCID mice injected with 231MFP breast cancer cells
Dosage:	50 mg/kg
Administration:	Intraperitoneal injection; daily; for 3 weeks
Result:	Significantly attenuated tumor growth in vivo.

体内研究

EN4 (50 mg/kg; intraperitoneal injection; daily; for 3 weeks) treatment significantly attenuated tumor growth in 231MFP breast tumor xenograft mice.

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

Animal Model:	SCID mice injected with 231MFP breast cancer cells
Dosage:	50 mg/kg
Administration:	Intraperitoneal injection; daily; for 3 weeks
Result:	Significantly attenuated tumor growth in vivo.

体内研究

EN4 (50 mg/kg; intraperitoneal injection; daily; for 3 weeks) treatment significantly attenuated tumor growth in 231MFP breast tumor xenograft mice.

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

Animal Model:	SCID mice injected with 231MFP breast cancer cells
Dosage:	50 mg/kg
Administration:	Intraperitoneal injection; daily; for 3 weeks
Result:	Significantly attenuated tumor growth in vivo.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (300.14 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4011 mL	12.0057 mL	24.0113 mL
5 mM	0.4802 mL	2.4011 mL	4.8023 mL
10 mM	0.2401 mL	1.2006 mL	2.4011 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 (protect from light)。-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: 2.08 mg/mL (4.99 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.99 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
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
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.08 mg/mL (4.99 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.99 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.99 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.99 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。