(Z)-4EGI-1
Based on 1 Customer Validation
(Z)-4EGI-1 is the Z-isomer of 4EGI-1 and is an inhibitor of eIF4E/eIF4G interaction and of translation initiation. (Z)-4EGI-1 effectively binds to eIF4E with an IC50 of 43.5 μM and a Kd value of 8.74 μM. (Z)-4EGI-1 has anticancer activity.
For research use only. We do not sell to patients.
- Purity: 98.0%
- CAS No.: 901787-88-0
- Formula: C18H12Cl2N4O4S
- Molecular Weight:451.28
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
eIF4 |
(Z)-4EGI-1 (15-30 μM; 6 hours; CRL-2813 melanoma cells) treatment markedly reduces the expressions of the regulatory proteins: cyclin D1, cyclin E, and Survivin, while the expressions of housekeeping proteins such as β-Actin and α-Tubulin are not affected[1].
(Z)-4EGI-1 inhibits cancer cells proliferation with IC50 values of 15.3 μM and 11.6 μM for CRL-2351 breast cells and CRL-2813 melanoma cells, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:CRL-2813 melanoma cells
-
Concentration:15 µM, 30 µM
-
Incubation Time:6 hours
-
Result:Markedly reduced the expressions of the regulatory proteins: cyclin D1, cyclin E, and Survivin.
Chemical Information
-
CAS No. 901787-88-0
-
Appearance Solid
-
Molecular Weight 451.28
-
Formula C18H12Cl2N4O4S
-
Color Light brown to gray
-
SMILES
O=C(O)/C(CC1=CC=CC=C1[N+]([O-])=O)=N/NC2=NC(C3=CC=C(Cl)C(Cl)=C3)=CS2
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 50 mg/mL (110.80 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.54 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
-
Data Sheet (276 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
References
[1]. Khuloud Takrouri, et al. Structure-activity Relationship Study of 4EGI-1, Small Molecule eIF4E/eIF4G Protein-Protein Interaction Inhibitors. Eur J Med Chem. 2014 Apr 22;77:361-77. [Content Brief]
[2]. Poornachandran Mahalingam, et al. Synthesis of Rigidified eIF4E/eIF4G inhibitor-1 (4EGI-1) Mimetic and Their in Vitro Characterization as Inhibitors of Protein-Protein Interaction. J Med Chem. 2014 Jun 26;57(12):5094-111. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2159 mL | 11.0796 mL | 22.1592 mL | 55.3980 mL |
| 5 mM | 0.4432 mL | 2.2159 mL | 4.4318 mL | 11.0796 mL | |
| 10 mM | 0.2216 mL | 1.1080 mL | 2.2159 mL | 5.5398 mL | |
| 15 mM | 0.1477 mL | 0.7386 mL | 1.4773 mL | 3.6932 mL | |
| 20 mM | 0.1108 mL | 0.5540 mL | 1.1080 mL | 2.7699 mL | |
| 25 mM | 0.0886 mL | 0.4432 mL | 0.8864 mL | 2.2159 mL | |
| 30 mM | 0.0739 mL | 0.3693 mL | 0.7386 mL | 1.8466 mL | |
| 40 mM | 0.0554 mL | 0.2770 mL | 0.5540 mL | 1.3849 mL | |
| 50 mM | 0.0443 mL | 0.2216 mL | 0.4432 mL | 1.1080 mL | |
| 60 mM | 0.0369 mL | 0.1847 mL | 0.3693 mL | 0.9233 mL | |
| 80 mM | 0.0277 mL | 0.1385 mL | 0.2770 mL | 0.6925 mL | |
| 100 mM | 0.0222 mL | 0.1108 mL | 0.2216 mL | 0.5540 mL |
(Z)-4EGI-1 Related Classifications
HY-19831A Related Classifications
Powered by Bioz