Tretazicar (CB1954)

製品コードS7829 バッチS782901

印刷

化学情報

Chemical Structure Synonyms NSC 115829 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C9H8N4O5
分子量 252.18 CAS No. 21919-05-1
Solubility (25°C)* 体外 DMSO 50 mg/mL (198.27 mM)
Water Insoluble
Ethanol Insoluble
* <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 Tretazicar (CB1954) is a anticancer prodrug that is converted in the presence of the enzyme NQO2 and co-substrate caricotamide ( EP-0152R) (EP) into a potent cytotoxic bifunctional alkylating agent. It can be activated by NAD(P)H quinone oxidoreductase 2.
in vitro The overexpression of nitroreductase oxidored nitro domain containing protein 1 (NOR1) is capable of converting the monofunctional alkylating agent CB1954 into a toxic form by reducing the 4 nitro group of CB1954 which is a potent cytotoxins. Toxic CB1954 enhances cells killing in the NPC cell line CNE1. the NOR1 gene enhances CB1954 mediated cell cytotoxicity through the upregulation of Grb2 expression and the activation of MAPK signal transduction in the HepG2 cell line[1].
in vivo The NTR/CB1954 system are used to specific ablation of cells in vivo. The effect of this inducible ablation system is dose-dependent[3]. NTR-mediated cell killing by CB1954 does not require cell proliferation. The activated CB1954 cross-links DNA which presumably triggers the apoptosis cascade, resulting in rapid cell death. specific and effective cells killing by NTR-CB1954 does not require a functional p53[2].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HepG2 Cells
濃度 4-10 μmol/L
反応時間 48 h
実験の流れ

The human hepatocellular carcinoma cells, HepG2 are maintained in RPMI 1640 supplemented with 10% fetal calf serum (FCS) in a humidified culture incubator at 37˚C with 5% CO2 and 95% air. Cell cyto-toxicity assays are conducted as previously described. HepG2 cells grown to ~80% confluence are washed with PBS and treated with a signal transduction inhibitor and/or CB1954. Measurements are collected from 10-12 individual microscopic fields in each experiment and data are summarized from 3-5 experiments.
動物実験 動物モデル RED 40 female mice expressing high levels of BLG-NTR transgene in the mammary gland and nontransgenic control mice on lactation day 6
投薬量 50 mg/kg
投与方法 i.p.

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。