| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
TLR7/8[1]
Telratolimod targets Toll-like receptor 7 (TLR7) and Toll-like receptor 8 (TLR8). It is a dual agonist. Activation of TLR7/8 on immune cells, such as dendritic cells, leads to the production of pro-inflammatory cytokines and type I interferons, which can stimulate an antitumor immune response. |
|---|---|
| ln Vitro |
Telratolimod (3M-052) is a TLR7/8 agonist with anticancer properties [1].
Telratolimod increases the production of IL-8 in HEK293 cells expressing human TLR7 or TLR8. It increases protein levels of IFN-α and TNF-α in isolated human peripheral blood mononuclear cells (PBMCs). This demonstrates its potent agonist activity. |
| ln Vivo |
When combined with CpG ODN, telratolimod (50 μg) more effectively slows tumor growth and decreases tumor volume in BALB/c mice harboring CT26 colon cancer cells. The combination of 200 μg of CpG ODN and 100 μg of telratolimod inhibits tumor growth and increases the longevity of mice with big tumors[1].
Telratolimod (50 μg) suppresses tumor volume and more potently blocks tumor growth in combination with CpG ODN in BALB/c mice bearing CT26 colon carcinoma cells. Its tissue-retained formulation allows for local TLR triggering without systemic cytokine release. |
| Enzyme Assay |
The activity of Telratolimod as a TLR7/8 agonist is assessed in cell-based reporter assays. HEK293 cells engineered to express human TLR7 or TLR8 and a reporter gene (e.g., NF-κB-driven luciferase) are used. The compound's potency (EC50) is determined by measuring reporter gene activation.
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| Cell Assay |
Cellular assays for Telratolimod involve treating human peripheral blood mononuclear cells (PBMCs) or dendritic cells with the compound and measuring the production of cytokines like IFN-α, TNF-α, and IL-8 by ELISA or multiplex assays. This confirms its immunostimulatory activity.
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| Animal Protocol |
In vivo efficacy is evaluated in immunocompetent mouse tumor models, such as the CT26 colon carcinoma model. Telratolimod is administered intratumorally or locally, and its effects on tumor growth, immune cell infiltration, and survival are assessed.
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| ADME/Pharmacokinetics |
Telratolimod is designed as a tissue-retained compound for local administration. It forms a depot at the injection site, allowing for gradual and sustained release. This limits systemic exposure and cytokine release. Its pharmacokinetic properties are tailored for this local delivery.
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| Toxicity/Toxicokinetics |
Toxicological data for Telratolimod is not detailed in the provided sources. As a clinical-stage compound, its safety has been evaluated in preclinical and clinical studies. Its local administration is designed to improve the safety profile by reducing systemic toxicity.
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| References | |
| Additional Infomation |
Telratolimod is a Toll-like receptor 7/8 (TLR7/8) agonist with potential immunostimulatory and antitumor activity. Upon intratumoral injection, Telratolimod binds to and activates TLR7 and TLR8, thereby stimulating antigen-presenting cells (APCs), including dendritic cells (DCs). Activation of DCs leads to the production of pro-inflammatory cytokines and activates the immune response of cytotoxic T lymphocytes (CTLs) and B lymphocytes. This may result in tumor cell lysis. TLR7 and TLR8 are members of the TLR family and play a crucial role in the activation of the immune system.
Telratolimod is a TLR7/8 agonist that has been investigated in clinical trials for cancer immunotherapy. Its tissue-retained formulation and sustained release profile are novel features designed to maximize local immune activation while minimizing systemic side effects. It represents a promising approach for treating solid tumors. |
| Molecular Formula |
C36H59N5O2
|
|---|---|
| Molecular Weight |
593.8860
|
| Exact Mass |
593.466
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| CAS # |
1359993-59-1
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| PubChem CID |
56833311
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| Appearance |
White to light yellow solid powder
|
| LogP |
11.9
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
25
|
| Heavy Atom Count |
43
|
| Complexity |
709
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O(CCCCNC(CCCCCCCCCCCCCCCCC)=O)N1C(CCCC)=NC2C(N)=NC3=CC=CC=C3C1=2
|
| InChi Key |
RRTPWQXEERTRRK-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C36H59N5O2/c1-3-5-7-8-9-10-11-12-13-14-15-16-17-18-19-27-33(42)38-28-22-23-29-43-41-32(26-6-4-2)40-34-35(41)30-24-20-21-25-31(30)39-36(34)37/h20-21,24-25H,3-19,22-23,26-29H2,1-2H3,(H2,37,39)(H,38,42)
|
| Chemical Name |
N-(4-((4-amino-2-butyl-1H-imidazo[4,5-c]quinolin-1-yl)oxy)butyl)stearamide
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| Synonyms |
Telratolimod 3M-052 MEDI 91973M 052 MEDI91973M052MEDI-9197
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~105.24 mM)
Ethanol : ~50 mg/mL (~84.19 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.21 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 900 μL of corn oil and mix evenly. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (3.50 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 2.08 mg/mL (3.50 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Solubility in Formulation 4: ≥ 2.08 mg/mL (3.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6838 mL | 8.4191 mL | 16.8381 mL | |
| 5 mM | 0.3368 mL | 1.6838 mL | 3.3676 mL | |
| 10 mM | 0.1684 mL | 0.8419 mL | 1.6838 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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