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Telratolimod TLR agonist

Cat.No.S9623

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 TLR agonist Chemical Structure

Chemical Structure

Molecular Weight: 593.89

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Quality Control

Batch: S962301 Ethanol]13 mg/mL]false]DMSO]Insoluble]false]Water]Insoluble]false Purity: 99.25%
99.25

Solubility

In vitro
Batch:

Ethanol : 13 mg/mL

DMSO : Insoluble
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Water : Insoluble

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Chemical Information, Storage & Stability

Molecular Weight 593.89 Formula
C36H59N5O2
Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1359993-59-1 -- Storage of Stock Solutions

Synonyms 3M-052, MEDI9197 Smiles CCCCCCCCCCCCCCCCCC(=O)NCCCCON1C(=NC2=C1C3=CC=CC=C3N=C2N)CCCC

Mechanism of Action

Targets/IC50/Ki
TLR7
TLR8
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.

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.

References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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