CVT-11127

製品コードS4470 バッチS447001

印刷

化学情報

 Chemical Structure Synonyms FMK13918 Storage
(From the date of receipt)
3 years -20°C powder
化学式

C25H23Cl2N5O3

分子量 512.39 CAS No. 1018674-83-3
Solubility (25°C)* 体外 DMSO 6 mg/mL (11.7 mM)
Water Insoluble
Ethanol Insoluble
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 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。

0.043mg/ml (0.08mM) Taking the 1 mL working solution as an example, add 50 μL of 0.86 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

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。

0.3mg/ml (0.59mM) Taking the 1 mL working solution as an example, add 50 μL of 6 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 CVT-11127 (FMK13918) はステアロイルCoAデサチュラーゼ-1 (SCD1)の阻害剤です。CVT-11127は、G(1)/S境界を介した細胞周期の進行を阻害し、プログラム細胞死を引き起こすことにより、脂質合成を減少し、増殖を阻害します。
in vitro

CVT-11127, an SCD1 inhibitor, decreases expression of SCD1, prevents the growth of STK11/KEAP1 co-mutant cells and sensitizes those cells to ferroptosis induction.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 H358 isogenic clones (NTC, STK11KO, KEAP1KO, DKO)
濃度 1 μM
反応時間 4 days
実験の流れ

3000 cells per well of the indicated genotype were plated in 96 well plates in triplicate for each drug dose. Cells were allowed to attach to the plate overnight in RPMI media supplemented with 10% FBS. Drug titrations were performed in full serum media in a separate 96 well plate with column 11 containing the highest dose of this compound, column 3 containing the lowest dose of this compound, and column 2 containing no drug. Outside wells were filled with PBS to avoid liquid precipitation. After cells were allowed to attached to the plate overnight, media was aspirated using a multi-channel aspirator, and replaced with drug media from the drug titration plates. Cells were inclubated at 37 degrees for 3–4 days as indicated. On the final day of drug treatment, media was once again aspirated using a multi-channel aspirator. Cells were washed 1× with PBS then fixed to the plate and stained with a solution of 0.5% crystal violet, 1% Methanol, and 1% Formaldehyde in PBS for 15 minutes at room temperature.

参考

  • https://pubmed.ncbi.nlm.nih.gov/20613975/
  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7722473/

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。