4EGI-1 is an inhibitor ofeIF4E/eIF4Ginteraction, with aK_dof 25 μM against eIF4E binding.

Kd: 25 μM (eIF4E/eIF4G)^[1]

4EGI-1 is an inhibitor of eIF4E/eIF4G interaction, with a K_dof 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^[1]. 4EGI-1 is cytotoxic to breast cancer cells, such as SKBR-3, MCF-7 and MDA-MB-231 cells, with the IC₅₀of appr 30 μM, and to the non-CSCs (Cancer stem cells), the IC₅₀is 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^[2]. 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^[3].

4EGI-1 (75 mg/kg, i.p.) inhibits breast cancer stem cells (CSC) tumor growth and tumorangiogenesis in vivo^[2]. 4EGI-1 (75 mg/kg, i.p.) shows inhibitory effect on the tumor volume and weight in mice bearing U87 cells^[3].

451.28

Solid

C₁₈H₁₂Cl₂N₄O₄S

315706-13-9

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 35 mg/mL(77.56 mM)

*"≥" means soluble, but saturation unknown.

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

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-CDin 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 μL20% 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