Telratolimod

Catalog No.S9623 Synonyms: 3M-052, MEDI9197

For research use only.

Telratolimod (3M-052, MEDI9197) is an agonist of toll-like receptor 7 (TLR-7) and toll-like receptor 8 (TLR-8) with antitumor activity.

Telratolimod Chemical Structure

CAS No. 1359993-59-1

Purity & Quality Control

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Biological Activity

Description Telratolimod (3M-052, MEDI9197) is an agonist of toll-like receptor 7 (TLR-7) and toll-like receptor 8 (TLR-8) with antitumor activity.
Targets
TLR7 [1] TLR8 [1]
In vitro

3M-052 induces both TNFα and IFNα in human PBMCs in a manner indicative of a dual TLR7/TLR8 agonist. 3M-052 stimulates the production of IL8 in HEK293 cells stably expressing either human TLR7 or TLR8. In contrast, no IL8 is stimulated in empty vector control cells. The TLR8 agonist activity of 3M-052 may be of particular value in the immunization of neonates and infants whose monocytes and antigen presenting cells have a diminished capacity to generate TH1 polarizing signals to TNFα and IFNα.[2]

In vivo

The co-administering CpG ODN with Telratolimod (3M-052) is remarkably effective at eliminating large established tumors and establishes long-term protective immunity. This anti-tumor activity is associated with a significant diminution in the frequency of tumor resident MDSC and accumulation of tumor-lytic NK and CD8 T cells, resulting in persistent anti-tumor immunity.[1]

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: PBMCs
  • Concentrations: 0.001 nM, 0.01 nM, 0.1 nM, 1 nM, 0.01 μM, 0.1 μM, 1 μM, 10 μM, 100 μM
  • Incubation Time: 16 h
  • Method:

    PBMC are cultured at 2 × 106/ml in 0.25 ml in 96-well plates. For evaluation of R848 and 3M-052, these compounds are first dissolved in DMSO and then diluted into culture medium to the final desired concentrations. DMSO concentration is maintained at 0.1% in all wells. The cultures are then incubated for 16 hr at 37 ◦C in a humidified atmosphere of 5.0% CO2 in air. The culture plates are then centrifuged to settle cells to the well surface and medium is removed for cytokine analysis by ELISA assay.

Animal Research:

[1]

  • Animal Models: 6–8-week-old BALB/c and C57BL/6 mice
  • Dosages: 50 μg, 100 μg (4 mg/ml)
  • Administration: intra tumor injection

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 593.89
Formula
C36H59N5O2
CAS No. 1359993-59-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCCCCCCCCCCCCCCCCC(=O)NCCCCON1C(=NC2=C1C3=CC=CC=C3N=C2N)CCCC

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02556463 Terminated Drug: MEDI9197|Biological: durvalumab Solid Tumors|CTCL|Cancer MedImmune LLC November 4 2015 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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