E104
Based on 1 Customer Validation
E104 is a selective Toll-like receptor 7 (TLR7) agonist. E104 promotes the release of pro-inflammatory factors and the polarization of macrophages toward the anti-tumor M1 phenotype by activating endosomal TLR7 and triggering downstream NF-κB and IRF signaling pathways. Antibody conjugates of E104 induce tumor regression. E104 can be used in research on pancreatic ductal adenocarcinoma and cancer.
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- Pureté : 99.38%
- CAS No.: 1610431-21-4
- Formule: C21H23N5
- Masse moléculaire:345.44
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
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TLR7 |
In Vitro
E104 (24 h) dose-dependently and potently induces TNF-α and IL-6 secretion in human peripheral blood mononuclear cells (human PBMCs) (EC50 = 163 nM and 36.7 nM) and human PBMC-derived M2 macrophages (EC50 = 183 nM and 143 nM)[2].
E104 effectively activates the TLR7/NF-κB signaling pathway in Ramos Blue cells, with an EC50 of 69 nM and a Cmax of 620 nM[4].
E104 (24 h) potently induces IL-6 secretion in mouse bone marrow-derived M2 macrophages (BMDM-M2) (EC50 = 65 nM) and mouse splenocytes (EC50 = 6.6 nM)[2].
E104 (16 nM-50 μM) potently activates NF-κB signaling in HEK 293 reporter cells expressing human TLR7, while showing no significant activation in cells expressing human TLR8 (indicating its high selectivity for TLR7)[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1610431-21-4
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Appearance Solid
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Masse moléculaire 345.44
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Formule C21H23N5
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Color White to light yellow
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SMILES
NC1=NC2=C(C=CC=C2)C3=C1N=C(CCCC)N3CC4=CC=C(C=C4)N
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 25 mg/mL (72.37 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.24 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Pureté et documentation
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Fiche technique (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[2]. Zhang A, et al. Nonglycosylated, Legumain-Cleavable ISACs Drive Potent Antitumor Immunotherapy via a Bystander Effect. Molecular cancer therapeutics. 2026 Apr 02;25(4):622-634. [Content Brief]
[4]. DeYoung EG, et al. Synthesis and Optimization of 1-Substituted Imidazo[4,5-c]quinoline TLR7 Agonists. ACS Med Chem Lett. 2023 Sep 14;14(10):1358-1368. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.8949 mL | 14.4743 mL | 28.9486 mL | 72.3715 mL |
| 5 mM | 0.5790 mL | 2.8949 mL | 5.7897 mL | 14.4743 mL | |
| 10 mM | 0.2895 mL | 1.4474 mL | 2.8949 mL | 7.2371 mL | |
| 15 mM | 0.1930 mL | 0.9650 mL | 1.9299 mL | 4.8248 mL | |
| 20 mM | 0.1447 mL | 0.7237 mL | 1.4474 mL | 3.6186 mL | |
| 25 mM | 0.1158 mL | 0.5790 mL | 1.1579 mL | 2.8949 mL | |
| 30 mM | 0.0965 mL | 0.4825 mL | 0.9650 mL | 2.4124 mL | |
| 40 mM | 0.0724 mL | 0.3619 mL | 0.7237 mL | 1.8093 mL | |
| 50 mM | 0.0579 mL | 0.2895 mL | 0.5790 mL | 1.4474 mL | |
| 60 mM | 0.0482 mL | 0.2412 mL | 0.4825 mL | 1.2062 mL |
E104 Related Classifications
HY-156174 Related Classifications
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