Tretazicar (CB1954)

製品コードS7829 バッチS782901

印刷

化学情報

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

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 1 40%PEG300 2 5%Tween80 3 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。	2.500mg/ml (9.91mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 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 1 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。	0.410mg/ml (1.63mM)	Taking the 1 mL working solution as an example, add 50 μL of 8.2 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	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 Tretazicar (CB1954) into a toxic form by reducing its 4-nitro group, resulting in a potent cytotoxin. This compound enhances cell 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/Tretazicar (CB1954) system is used for specific ablation of cells in vivo. The effect of this inducible ablation system is dose-dependent^[3]. NTR-mediated cell killing by this compound does not require cell proliferation. The activated form cross-links DNA which presumably triggers the apoptosis cascade, resulting in rapid cell death. Specific and effective cell 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 Tretazicar (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.

参考

https://pubmed.ncbi.nlm.nih.gov/23741254/
https://pubmed.ncbi.nlm.nih.gov/10505099/
https://pubmed.ncbi.nlm.nih.gov/12429046/

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：

Reporter cell lines to screen for inhibitors or regulators of the KRAS-RAF-MEK1/2-ERK1/2 pathway [ Biochem J, 2024, 481(6):405-422]	PubMed: 38381045

Reporter cell lines to screen for inhibitors or regulators of the KRAS-RAF-MEK1/2-ERK1/2 pathway [ Biochem J, 2024, 481(6):405-422]

PubMed: 38381045

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。