| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
eIF4
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|---|---|
| ln Vitro |
Housekeeping proteins like β Expression - actin and α-tubulin are unaffected by (Z)-4EGI-1 (15-30 μM; 6 hr; CRL-2813 melanoma cells) treatment, however the expression of regulatory proteins including cyclin D1, cyclin E, and survivin was drastically reduced [1]. With IC50 values of 15.3 μM and 11.6 μM for CRL-2351 breast cells and CRL-2813 melanoma cells, respectively, (Z)-4EGI-1 suppresses the growth of cancer cells [2].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: CRL-2813 melanoma cells Tested Concentrations: 15 µM, 30 µM Incubation Duration: 6 hrs (hours) Experimental Results: Markedly decreased the expressions of the regulatory proteins: cyclin D1, cyclin E, and Survivin. |
| 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.
[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. |
| Molecular Formula |
C18H12CL2N4O4S
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|---|---|
| Molecular Weight |
451.28
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| CAS # |
901787-88-0
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| Related CAS # |
4EGI-1;315706-13-9
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| SMILES |
N(C1SC=C(C2C=CC(Cl)=C(Cl)C=2)N=1)/N=C(\C(=O)O)/CC1C=CC=CC=1[N+](=O)[O-]
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| Solubility (In Vitro) |
DMSO : 50 mg/mL (110.80 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.54 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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