4EGI-1|cas:315706-13-9|西域试剂

4EGI-1,99.91%

产品编号：Bellancom-19831| CAS NO：315706-13-9| 分子式：C₁₈H₁₂Cl₂N₄O₄S| 分子量：451.28

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-19831	￥990.00	杭州北京（现货）
Bellancom-19831	￥1300.00	杭州北京（现货）
Bellancom-19831	￥2400.00	杭州北京（现货）
Bellancom-19831	￥3500.00	杭州北京（现货）
Bellancom-19831	￥5800.00	杭州北京（现货）

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4EGI-1

产品介绍

4EGI-1 是一种 eIF4E/eIF4G 相互作用抑制剂，抑制 eIF4E 结合，K_d 值为 25 μM。

生物活性

4EGI-1 is an inhibitor of eIF4E/eIF4G interaction, with a K_d of 25 μM against eIF4E binding.

体外研究

4EGI-1 is an inhibitor of eIF4E/eIF4G interaction, with a K_d of 25 μM against eIF4E binding. 4EGI-1 disrupts the eIF4F complex and inhibits expression of oncogenic proteins in mammalian cells. 4EGI-1 (0-40 μM) also exhibits proapoptotic activity and inhibits the growth of multiple cancer cell lines. 4EGI-1 is cytotoxic to breast cancer cells, such as SKBR-3, MCF-7 and MDA-MB-231 cells, with the IC₅₀ of appr 30 μM, and to the non-CSCs (Cancer stem cells), the IC₅₀ is about 22 μM. 4EGI-1 enhances breast CSC differentiation (40 μM), and suppresses breast CSC induced HUVEC tube-like structure formation (8 μM). Moreover, 4EGI-1 selectively inhibits translation that persists in CSC maintenance and dissemination. 4EGI-1 (50 µM) impairs the formation of eIF4F complex in U87 cells. 4EGI-1 (10, 50 and 100 µM) inhibits cell proliferation via inducing apoptosis in U87 cells, and the apoptosis is via Bax activation. 4EGI-1 causes mitochondrial dysfunction, and induces ER stress via GRP-78 activation, in U87 cells.

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

体内研究

4EGI-1 (75 mg/kg, i.p.) inhibits breast cancer stem cells (CSC) tumor growth and tumorangiogenesis in vivo. 4EGI-1 (75 mg/kg, i.p.) shows inhibitory effect on the tumor volume and weight in mice bearing U87 cells.

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 : ≥ 35 mg/mL (77.56 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2159 mL	11.0796 mL	22.1592 mL
5 mM	0.4432 mL	2.2159 mL	4.4318 mL
10 mM	0.2216 mL	1.1080 mL	2.2159 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 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (5.54 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (5.54 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 25.0 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