Trifluridine (NSC 75520)

製品コードS1778 バッチS177806

印刷

化学情報

Chemical Structure Synonyms NSC 529182, NSC 75520, Viroptic, Trifluorothymidine, TFT Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C10H11F3N2O5
分子量 296.2 CAS No. 70-00-8
Solubility (25°C)* 体外 DMSO 59 mg/mL (199.18 mM)
Water (warmed with 50ºC water bath) 30 mg/mL (101.28 mM)
Ethanol 30 mg/mL (101.28 mM)
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 2.950mg/ml (9.96mM) Taking the 1 mL working solution as an example, add 50 μL of 59 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. 
Clear solution
5% DMSO 95% Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 0.730mg/ml (2.46mM) Taking the 1 mL working solution as an example, add 50 μL of 14.6 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. 
* <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 Trifluridine（NSC 529182、NSC 75520、Viroptic、Trifluorothymidine、TFT）は、ウイルスのDNA複製と相互作用する抗ヘルペスウイルス薬であり、主に眼に使用されます。
in vitro Trifluridine (NSC 75520) inhibits proliferations of mouse bone marrow cells and human colorectal carcinoma cells implanted to nude mice dose-dependently. It also inhibits colony formation of bone marrow cells in a concentration-dependent manner. This compound and 2'-deoxy-5-fluorouridine (FdUrd) are incorporated into DNA with different efficiencies due to differences in the substrate specificities of TK1 and DUT, causing abundant FTD incorporation into DNA. FTD-treated cells shows differing nuclear morphologies compared to FdUrd-treated cells. It further inhibits proliferations of mouse bone marrow cells and human colorectal carcinoma cells implanted to nude mice dose-dependently.
in vivo Trifluridine (NSC 75520) has significantly fewer swabs positive for HSV-1 than the untreated eyes in the infected rabbits. This compound has increased antitumor activity and is incorporated into DNA more effectively than continuously infused Trifluridine in mice. It gradually accumulates in tumor cell DNA, in a TPI-independent manner, and significantly delays tumor growth and prolonged survival in mice, compared to treatment with 5-FU derivatives. Furthermore, it results in significantly lower viral titers, fewer HSV-1-positive eyes/total during the treatment period, lower keratitis scores, fewer eyes with keratitis/total, and a shorter time to resolution of keratitis in the New Zealand rabbit ocular model.

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/26084259/
  • https://pubmed.ncbi.nlm.nih.gov/25901475/
  • https://pubmed.ncbi.nlm.nih.gov/24018612/
  • https://pubmed.ncbi.nlm.nih.gov/2539342/
  • https://pubmed.ncbi.nlm.nih.gov/25230742/
  • https://pubmed.ncbi.nlm.nih.gov/9950596/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Codon-specific KRAS mutations predict survival benefit of trifluridine/tipiracil in metastatic colorectal cancer [ Nat Med, 2023, 29(3):605-614] PubMed: 36864254
Culture media composition influences patient-derived organoid ability to predict therapeutic responses in gastrointestinal cancers [ JCI Insight, 2022, 7(22e158060)] PubMed: 36256477
Trifluridine induces HUVECs senescence by inhibiting mTOR-dependent autophagy [ Biochem Biophys Res Commun, 2022, 610:119-126] PubMed: 35462092
Intracellular H2S production is an autophagy-dependent adaptive response to DNA damage [ Cell Chem Biol, 2021, S2451-9456(21)00261-0] PubMed: 34166610
Standalone or combinatorial phenylbutyrate therapy shows excellent antiviral activity and mimics CREB3 silencing [ Sci Adv, 2020, 6(49)eabd9443] PubMed: 33277262
Prior inhibition of AKT phosphorylation by BX795 can define a safer strategy to prevent herpes simplex virus-1 infection of the eye. [ Ocul Surf, 2019, 10.1016/j.jtos.2019.11.011] PubMed: 31770600
Effect of RAD51C expression on the chemosensitivity of Eμ-Myc p19Arf-/- cells and its clinical significance in breast cancer [ Oncol Lett, 2018, 15(5):6107-6114] PubMed: 29731842
Targeting Herpes Simplex Virus-1 gD by a DNA Aptamer Can Be an Effective New Strategy to Curb Viral Infection [ Mol Ther Nucleic Acids, 2017, 9:365-378] PubMed: 29246315

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。