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Telratolimod (MEDI9197, MEDI-9197, 3M-052) is a novel and potent agonist of toll-like receptor 7/8 (TLR-7/8) with the potential for the treatment of solid tumors. Telratolimod is an IRM bearing a C18 lipid moiety and designed for slow dissemination from the site of application. MEDI-9197 drives a strong Th1 response to hemagglutinin and serum neutralization of viable H1N1 A/Puerto Rico/8/34 virus in the absence of circulating TNFα or the induction of Th1 cytokines.
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| ln Vitro |
Telratolimod (3M-052) is a TLR7/8 agonist with anticancer properties [1].
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| 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].
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| References | ||
| Additional Infomation |
Telratolimod is a toll-like receptor type 7 and 8 (TLR7/8) agonist with potential immunostimulating and antitumor activities. Upon intratumoral administration, telratolimod binds to and activates TLR7 and 8, thereby stimulating antigen-presenting cells (APCs), including dendritic cells (DCs). Activation of DCs results in the production of proinflammatory cytokines, and the activation of cytotoxic T-lymphocyte (CTL) and B-lymphocyte immune responses. This may cause tumor cell lysis. TLR7 and 8, members of the TLR family, play fundamental roles in the activation of the immune system.
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| Molecular Formula |
C36H59N5O2
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|---|---|
| Molecular Weight |
593.8860
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| 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
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| LogP |
11.9
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
25
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| Heavy Atom Count |
43
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| Complexity |
709
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(CCCCNC(CCCCCCCCCCCCCCCCC)=O)N1C(CCCC)=NC2C(N)=NC3=CC=CC=C3C1=2
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| InChi Key |
RRTPWQXEERTRRK-UHFFFAOYSA-N
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| 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)
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| 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)
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| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~105.24 mM)
Ethanol : ~50 mg/mL (~84.19 mM) |
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| 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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