DSR-6434
Based on 1 publication(s) in Google Scholar
DSR-6434 is a potent and selective Toll-like receptor 7 (TLR7) agonist, with EC50s of 7.2 nM and 4.6 nM for human and mice TLR7, respectively. DSR-6434 has a strong antitumor effect.
For research use only. We do not sell to patients.
- Purity: 99.32%
- CAS No.: 1059070-10-8
- Formula: C19H28N8O2
- Molecular Weight:400.48
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) DSR-6434
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Biological Activity
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TLR7 7.2 nM (EC50, Human) |
TLR7 4.6 nM (EC50, Mice) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
7.2 nM
Compound: 20, DSR-6434
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Agonist activity at human TLR7 expressed in HEK293 cells by NFkappaB SEAP reporter gene assay
Agonist activity at human TLR7 expressed in HEK293 cells by NFkappaB SEAP reporter gene assay
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[PMID: 23265901] |
To assess the specificity of DSR-6434 toward TLR7, an NF-κB-driven reporter assay is performed in HEK293 cells engineered to express either hTLR7, TLR8 or TLR9. In this assay, successful binding of DSR-6434 to the specific receptor leads to NF-κB activation. DSR-6434 is capable of stimulating reporter gene activity only in HEK293 cells expressing hTLR7 and not in HEK293 cells expressing the structurally similar hTLR8 or hTLR9[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:B6C3F1 mice injected with HM-1 ovarian cancer cells[1]
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Dosage:0.1 mg/kg, 1 mg/kg
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Administration:Intravenous injection; biweekly; for 4 weeks
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Result:Suppressed the lung metastasis significantly, 78% inhibition was seen at 0.1 mg/kg dosing (with no tumor metastasis at the 1 mg/kg group).
Chemical Information
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CAS No. 1059070-10-8
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Appearance Solid
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Molecular Weight 400.48
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Formula C19H28N8O2
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Color Light yellow to yellow
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SMILES
O=C1N(C2=NC(NCCCC)=NC(N)=C2N1)CC3=CN=C(OCCN(C)C)C=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
DMSO : 125 mg/mL (312.13 mM; Need ultrasonic; 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)
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: ≥ 1 mg/mL (2.50 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
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.
Purity & Documentation
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Data Sheet (272 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)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Nakamura T, et al. Synthesis and evaluation of 8-oxoadenine derivatives as potent Toll-like receptor 7 agonists with high water solubility. Bioorg Med Chem Lett. 2013 Feb 1;23(3):669-72. [Content Brief]
[2]. Adlard AL, et al. A novel systemically administered Toll-like receptor 7 agonist potentiates the effect of ionizing radiation in murine solid tumor models. Int J Cancer. 2014 Aug 15;135(4):820-9. [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, 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 | 2.4970 mL | 12.4850 mL | 24.9700 mL | 62.4251 mL |
| 5 mM | 0.4994 mL | 2.4970 mL | 4.9940 mL | 12.4850 mL | |
| 10 mM | 0.2497 mL | 1.2485 mL | 2.4970 mL | 6.2425 mL | |
| 15 mM | 0.1665 mL | 0.8323 mL | 1.6647 mL | 4.1617 mL | |
| 20 mM | 0.1249 mL | 0.6243 mL | 1.2485 mL | 3.1213 mL | |
| 25 mM | 0.0999 mL | 0.4994 mL | 0.9988 mL | 2.4970 mL | |
| 30 mM | 0.0832 mL | 0.4162 mL | 0.8323 mL | 2.0808 mL | |
| 40 mM | 0.0624 mL | 0.3121 mL | 0.6243 mL | 1.5606 mL | |
| 50 mM | 0.0499 mL | 0.2497 mL | 0.4994 mL | 1.2485 mL | |
| 60 mM | 0.0416 mL | 0.2081 mL | 0.4162 mL | 1.0404 mL | |
| 80 mM | 0.0312 mL | 0.1561 mL | 0.3121 mL | 0.7803 mL | |
| 100 mM | 0.0250 mL | 0.1249 mL | 0.2497 mL | 0.6243 mL |
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