TBK1/IKKε-IN-5
Based on 2 publication(s) in Google Scholar
TBK1/IKKε-IN-5 (compound 1) is an orally active TBK1 and IKKε dual inhibitor, with IC50 values of 1 and 5.6 nM, respectively. TBK1/IKKε-IN-5 enhances the blockade response to PD-1 and induces immune memory in rats when combines with anti-PD-L1. TBK1/IKKε-IN-5 can be used in cancer research, especially in tumour immunity.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.96%
- No. CAS: 1893397-65-3
- Fòrmula: C28H31N7O3
- Peso molecular:513.59
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) TBK1/IKKε-IN-5
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Actividad biológica
Descripciòn
IC50 & Target
IC50: 1 nM (TBK1), 5.6 nM (IKKε)[1].
In Vitro
TBK1/IKKε-IN-5 (0.001-10 μM; 24 or 96 h) promotess secretion of IL-2 and IFN-γ in purified CD4+ and CD8+ T cells and IL-2 in Jurkat human T-cell leukemia cells[1].
TBK1/IKKε-IN-5 effectively blocks immune suppressive cytokine elaboration by CT26 cell line spheroids, without cytotoxic effects[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CD4+ and CD8+ T cells, Jurkat T cell leukemia cells
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Concentration:0.001-10 µM
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Incubation Time:24 h (for IL-2); 96 h(for IFN-γ)
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Result:Enhanced secretion of IL-2 and IFN-γ.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Balb/c mice (11 to 12-week-old; bearing CT26 tumors)[1].
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Dosage:40 mg/kg
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Administration:Oral gavage; single daily for 26 days (combine with anti-PD-L1).
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Result:Exhibited greater tumor control and longer survival when combined with anti-PD-L1 than used alone of both agents
Induced immunologic memory of CT26 cells in mice when combined with anti-PD-L1.
Chemical Information
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No. CAS 1893397-65-3
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Appearance Solid
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Peso molecular 513.59
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Fòrmula C28H31N7O3
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Color Light yellow to yellow
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SMILES
N#CC1=CC(C2=NC(NC3=CC=C(N4CCN(C5COC5)CC4)C=C3)=NC=N2)=CC=C1OC6CCOCC6
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
Solvente y solubilidad
In Vitro:
DMSO : 6.67 mg/mL (12.99 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.67 mg/mL (1.30 mM); Clear solution
This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9471 mL | 9.7354 mL | 19.4708 mL | 48.6770 mL |
| 5 mM | 0.3894 mL | 1.9471 mL | 3.8942 mL | 9.7354 mL | |
| 10 mM | 0.1947 mL | 0.9735 mL | 1.9471 mL | 4.8677 mL |
TBK1/IKKε-IN-5 Related Classifications
HY-128679 Related Classifications
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