Home Immunology & Inflammation TLR agonist Telratolimod For research use only.

Telratolimod

Synonyms: 3M-052, MEDI9197

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

Telratolimod Chemical Structure

CAS No. 1359993-59-1

Purity & Quality Control

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

Telratolimod Related Products

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
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models 6–8-week-old BALB/c and C57BL/6 mice
Dosages 50 μg, 100 μg (4 mg/ml)
Administration intra tumor injection
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02556463 Terminated
Solid Tumors|CTCL|Cancer
MedImmune LLC
 November 4 2015 Phase 1

Chemical Information & Solubility

Molecular Weight 593.89 Formula
C36H59N5O2
CAS No. 1359993-59-1 SDF --
Smiles CCCCCCCCCCCCCCCCCC(=O)NCCCCON1C(=NC2=C1C3=CC=CC=C3N=C2N)CCCC
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

Ethanol : 13 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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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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