Conditionnement : 5mg
Téléphone : +1 850 650 7790
Synonyms: IKE
| Description | Imidazole ketone erastin (IKE) is an ferroptosis inducer with inhibitory effects on system Xc-cystine/glutamate transporter proteins. Imidazole ketone erastin has antitumor activity and induces glutathione depletion and lipid peroxidation. |
| Targets & IC50 | DLBCL cells:> 10 μM, DLBCL cells:100 nM-10 μM, system xc:30 nM |
| In vitro | METHODS: Human astrocytoma cells CCF-STTG1 were incubated with Imidazole ketone erastin for 2 h. Glutamate released into the medium was detected using glutamate oxidase, horseradish peroxidase, and Amplex UltraRed fluorimetric assay. RESULTS: The IC50 for system xc- inhibition by Imidazole ketone erastin was 30 nM. [1] METHODS: 18 DLBCL cell lines were treated with Imidazole ketone erastin (0.0001-100 µM) for 24 h. Cell viability was measured using the Cell Titor-Glo luminescent cell viability test. RESULTS: DLBCL cell lines showed different sensitivities to Imidazole ketone erastin inhibition. 7 cell lines with IC50 <100 nM were categorized as sensitive; 5 cell lines with IC50 >10 µM were categorized as resistant; and 6 cell lines with IC50 between 100 nM and 10 µM were categorized as moderately resistant. [2] |
| In vivo | METHODS: To detect anti-tumor activity in vivo, Imidazole ketone erastin (23-40 mg/kg, 5% DMSO in HBSS at pH 4) was injected intraperitoneally into NCG mice harboring human diffuse histiocytic lymphoma SUDHL6 once daily for thirteen days. RESULTS: Imidazole ketone erastin inhibited tumor growth in vivo. [2] METHODS: To test the antitumor activity in vivo, Imidazole ketone erastin (40 mg/kg every two days) and liproxstatin-1 (10 mg/kg once a day) were intraperitoneally injected into C57BL/6 mice with the hepatocellular carcinoma tumor Hepa1-6 for ten days on either a control (Met+) or a methionine-free (Met-) diet. Met-) diet. RESULTS: In mice receiving the control diet, Imidazole ketone erastin treatment effectively reduced tumor growth, and this effect was completely blocked by liproxtatin-1. However, in mice receiving a methionine-free diet, Imidazole ketone erastin treatment failed to inhibit tumor growth. [3] |
| Synonyms | IKE |
| Molecular Weight | 655.14 |
| Formula | C35H35ClN6O5 |
| Cas No. | 1801530-11-9 |
| Smiles | CC(C)Oc1ccc(cc1-n1c(CN2CCN(CC2)C(=O)COc2ccc(Cl)cc2)nc2ccccc2c1=O)C(=O)Cn1ccnc1 |
| Relative Density. | 1.34 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: 100 mg/mL (152.64 mM), Sonication and heating are recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (6.11 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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