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Purity: ≥98%
4EGI-1 is a potent and competitive eIF4E/eIF4G interaction inhibitor which binds to eIF4E with KD of 25 μM. It has been demonstrated that 4EGI-1, through down-regulating FLIPS/L and inducing DR5, amplifies TRAIL (tumor necrosis factor-related apoptosis-inducing ligand)-induced apoptosis. These properties of the compound appear to be unrelated to its capacity to suppress cap-dependent protein translation, which is brought about by binding to eIF4E and disrupting the eIF4E/eIF4G association. Research has demonstrated that although 4EGI-1 separates eIF4G from eIF4E, it also strengthens the 4E-BP association in vitro and in vivo.
| Targets |
eIF4E/eIF4G (Kd = 25 μM); mTOR
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| ln Vivo |
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| Cell Assay |
For a duration of 24 hours, DMSO, [E]-4EGI-1, or [Z]-4EGI-1 at various concentrations are applied to 1 × 104 breast CSCs HMLER (CD44high/CD24low)FA cells and other indicated breast cancer cells. Cell viability assays are carried out on the cells using a cell viability assay kit. Three separate experiments are carried out. The mean ± SD, t-test, two-tailed, average IC50 results are displayed[2].
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| Animal Protocol |
Mice: For the tumor xenografted assay, 100 μL of a Matrigel/DMEM mixture (Matrigel: DMEM = 1:2) is combined with 1×105 breast cancer stem cells (CSCs). Subcutaneous injections of breast CSCs, Matrigel, and DMEM mixtures are administered to the mammary glands of NOD/SCID female mice. Following the formation of the tumor, which grew to a volume of approximately 75 mm3 and affected 5 mice per group, the mice were given intraperitoneal injections of DMSO, 75 mg/kg [E]-4EGI-1, or 75 mg/kg [Z]-4EGI-1 every day for 30 days. Three-day intervals are used to measure tumor volumes. Mice are sacrificed on day thirty, and tumors are removed. Weights of tumors are quantified. Western blot, immunoprecipitation, and immunohistochemistry analyses are performed on tumor tissue samples[2].
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| References |
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| Molecular Formula |
C18H12CL2N4O4S
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| Molecular Weight |
451.28
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| Exact Mass |
450.00
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| Elemental Analysis |
C, 47.91; H, 2.68; Cl, 15.71; N, 12.42; O, 14.18; S, 7.10
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| CAS # |
315706-13-9
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| Related CAS # |
(Z)-4EGI-1;901787-88-0
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| Appearance |
Solid powder
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| SMILES |
C1=CC=C(C(=C1)C/C(=N\NC2=NC(=CS2)C3=CC(=C(C=C3)Cl)Cl)/C(=O)O)[N+](=O)[O-]
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| InChi Key |
KFRKRECSIYXARE-HYARGMPZSA-N
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| InChi Code |
InChI=1S/C18H12Cl2N4O4S/c19-12-6-5-10(7-13(12)20)15-9-29-18(21-15)23-22-14(17(25)26)8-11-3-1-2-4-16(11)24(27)28/h1-7,9H,8H2,(H,21,23)(H,25,26)/b22-14+
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| Chemical Name |
(2E)-2-[[4-(3,4-dichlorophenyl)-1,3-thiazol-2-yl]hydrazinylidene]-3-(2-nitrophenyl)propanoic acid
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| Synonyms |
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| HS Tariff Code |
2934.99.03.00
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| 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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