ZZW-115

製品コードE1037 バッチE103701

印刷

化学情報

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

C₂₄H₃₄Cl₃F₃N₄S

分子量 573.97 CAS No. 10122-45-9
Solubility (25°C)* 体外 DMSO 93 mg/mL (162.02 mM)
Water 46 mg/mL (80.14 mM)
Ethanol 2 mg/mL (3.48 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。

1.160mg/ml (2.02mM) Taking the 1 mL working solution as an example, add 50 μL of 23.2 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。

1.160mg/ml (2.02mM) Taking the 1 mL working solution as an example, add 50 μL of 23.2 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 ZZW-115 is a potent NUPR1 inhibitor with IC50s of 0.42 μM in Hep2G cells and 7.75 μM in SaOS-2 cells. ZZW-115 shows evident antitumor activity through its interaction with NUPR1.
in vitro

ZZW-115 is capable of efficiently killing the pancreatic tumor cell lines by targeting NUPR1 and inhibits the growth of other tumor-derived cells. This compound induced cell death is the consequence of a decrease of ATP production by the mitochondria accompanied by an increase of mitochondrial ROS production with a transient metabolic shift toward anaerobic glycolysis inhibiting.[1]

in vivo

ZZW-115 can disrupt tumor growth at low doses and can reduce tumor size for the xenografted tumors, without obvious neurological side effects in the mice. This compound is a very efficient anticancer drug candidate in vivo on mice because, due mainly to necrosis, it is capable not only of stopping tumor growth but also of decreasing the tumor size until its disappearance.[1]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Panc-1 cells
濃度 0 μM - 100 μM
反応時間 24 h, 72 h
実験の流れ

Cells are plated in 96-well plates. Twenty-four hours later, the media are supplemented with 0–100 μM concentration of ZZW-115, and are incubated for another additional 24 or 72 hours. Cell viability is estimated after addition of the CellTiter-Blue viability reagent (Promega) for 3 hours according to the protocol provided by the supplier. Cell viability the concernings normalized with respect to untreated cell rates.

動物実験 動物モデル NMRI-Foxn1nu/Foxn1nu mice
投薬量 5 mg/kg
投与方法 s.c.

参考

  • https://pubmed.ncbi.nlm.nih.gov/30920390/

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。