Telratolimod

Catalog No.S9623 Batch:S962301

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Technical Data

Formula
C36H59N5O2
Molecular Weight 593.89 CAS No. 1359993-59-1
Solubility (25°C)* In vitro Ethanol 13 mg/mL (21.88 mM)
DMSO Insoluble
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% ethyl alcohol 95% Corn oil
0.65mg/ml Taking the 1 mL working solution as an example, add 50 μL of 13 mg/ml clear ethyl alcohol stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%ethyl alcohol 40%PEG300 5%Tween80 50%ddH2O
0.325mg/ml Taking the 1 mL working solution as an example, add 50 μL of 6.5 mg/ml clarified ethyl alcohol stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:

[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 Study:

[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

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.