Fluzoparib (SHR-3162)

製品コードS9712 バッチS971201

印刷

化学情報

Chemical Structure Synonyms HS10160 Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C22H16F4N6O2
分子量 472.40 CAS No. 1358715-18-0
Solubility (25°C)* 体外 DMSO 94 mg/mL (198.98 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）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 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 Corn oil
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 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

Fluzoparib (SHR3162, HS10160) is a potent Poly (ADP-ribose) polymerase (PARP) inhibitor that shows anti-tumor activity with an IC50 of 1.46±0.72 nM for PARP1.
in vitro

All four NSCLC cell lines (A549, H460, H1299, and PC9) shows decreased viability upon exposure to fluzoparib, and the effect is time and dose dependent. Fluzoparib acts synergistically to inhibit cell growth and promote apoptosis among lung cancer cells.[2]
in vivo

An H460 cell xenograft mouse model is established to study the in vivo effects of fluzoparib and RT on tumor growth and survival. Treatment with RT + fluzoparib more effectively delayed tumor growth than treatment with either RT or fluzoparib individually. When combined with RT, fluzoparib conferres a significant survival benefit with no evidence of toxicity.[2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 human NSCLC cell lines A549, H460, H1299 and PC9
濃度 0–800 μM
反応時間 24 h, 48 h, 72 h, 96 h
実験の流れ

Cells of all four NSCLC cell lines (A549, H460, H1299 and PC9) are plated in 96-well plates separately, with approximately 2 × 103 cells added to each well. The cells are exposed to fluzoparib at different concentration (0–800 μM) in completed medium for 24, 48, 72, or 96 h. After exposure of the cells to fluzoparib for the indicated time period, the CellTiter 96 Aqueous Non-radioactive Cell Proliferation assay is used to detect cell viability, and IC50 values are calculated. The experiment is performed three times and mean and standard deviation (SD) values are calculated for further statistical analysis of the results.
動物実験 動物モデル 5-6 week-old female Nu/Nu mice
投薬量 1 mg/kg
投与方法 IG

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：

Slow Dissociation from the PARP1-HPF1 Complex Drives Inhibitor Potency [ Biochemistry, 2023, 62(16):2382-2390] PubMed: 37531469

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。