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Synonyms: eFT226, eFT 226
| Description | Zotatifin (eFT226) is a selective eIF4A inhibitor with antiviral and anticancer activities, blocking tumor growth driven by receptor tyrosine kinases and inhibiting Sox4 translation, inducing apoptosis. |
| Targets & IC50 | eIF4A:2 nM |
| In vitro | Methods: Zotatifin (0.0001 μM-1 μM, 72 hours) was used to treat MDA-MB-231 cells, and the antiproliferative activity was determined. Results: Zotatifin showed potent antiproliferative activity in MDA-MB-231 tumor cells, with a GI50 value of less than 15 nM. TMD8 and Pfeiffer DLBCL tumor cells were treated with Zotatifin (30 μM-100 μM, 3 or 24 hours), and the changes in protein levels were detected by WB. Results: Zotatifin reduced the expression of MYC, CCND3, BCL2, and MCL1 proteins in a time- and dose-dependent manner.[1] |
| In vivo | Methods: Zotatifin (1 mg/kg, intravenous injection, 14-22 days) was used to treat mice bearing TMD8 xenografts, HBL1 xenografts, Pfeiffer xenografts, SU-DHL-6 xenografts, SU-DHL-10 xenografts, and Ramos xenografts, and the tumor inhibition rate was observed. Results: The tumor growth percentages of various tumor xenograft model mice after Zotatifin treatment were 97%, 87%, 70%, 83%, 37%, and 75%, respectively. Methods: Zotatifin (0.001 mg/kg-1 mg/kg, intravenous injection; 15 days) was used to treat mice bearing B-cell lymphoma xenograft models, and the tumor growth in vivo was observed. Results: Zotatifin inhibited the growth of B-cell lymphoma xenografts and was well tolerated in B-cell lymphoma xenograft models in vivo.[2] |
| Synonyms | eFT226, eFT 226 |
| Molecular Weight | 487.55 |
| Formula | C28H29N3O5 |
| Cas No. | 2098191-53-6 |
| Smiles | O[C@]12[C@]([C@@H]([C@@H](CN(C)C)[C@H]1O)C3=CC=CC=C3)(OC=4C2=C(OC)N=C(OC)C4)C5=CC=C(C#N)C=C5 |
| Relative Density. | 1.36 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 150 mg/mL (307.66 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (10.26 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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