Telratolimod

製品コードS9623 バッチS962301

印刷

化学情報

Chemical Structure Synonyms 3M-052, MEDI9197 Storage
(From the date of receipt)		 3 years -20°C powder
化学式
C36H59N5O2
分子量 593.89 CAS No. 1359993-59-1
Solubility (25°C)* 体外 Ethanol 13 mg/mL (21.88 mM)
DMSO Insoluble
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5% DMSO 95% Corn oil
0.65mg/ml Taking the 1 mL working solution as an example, add 50 μL of 13 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 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 DMSO 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.

溶剤液（一定の濃度）を調合する

生物活性

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

プロトコル(参考用のみ)

細胞アッセイ 細胞株 PBMCs
濃度 0.001 nM, 0.01 nM, 0.1 nM, 1 nM, 0.01 μM, 0.1 μM, 1 μM, 10 μM, 100 μM
反応時間 16 h
実験の流れ

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.
動物実験 動物モデル 6–8-week-old BALB/c and C57BL/6 mice
投薬量 50 μg, 100 μg (4 mg/ml)
投与方法 intra tumor injection

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。