COTI-2

製品コードS8580 バッチS858001

印刷

化学情報

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

C19H22N6S
分子量 366.48 CAS No. 1039455-84-9
Solubility (25°C)* 体外 DMSO 6.25 mg/mL (17.05 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.
* <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 COTI-2 is an orally available third generation thiosemicarbazone and activator of mutant forms of the p53 protein, with potential antineoplastic activity.
in vitro The thiosemicarbazone COTI-2 is reported to promote refolding of mutant p53 and restore wild-type-p53 function. It is active against human tumour cell lines of various origins at nanomolar concentrations, induces cell death by apoptosis[1]. This compound is highly efficacious against multiple cancer cell lines from a broad range of human cancers both in vitro and in vivo. It does not significantly inhibit over 200 kinases from major kinase pathways involved in cancer that were evaluated in both kinase assays and does not inhibit the ATPase activity of Hsp90, a ubiquitous molecular chaperone that plays an essential role in cell survival and cell cycle control[2].
in vivo COTI-2 significantly inhibited tumor growth in the HT-29 human colorectal tumor xenografts at a dose of 10 mg/kg. This compound also significantly inhibited tumor growth in the SHP-77 SCLC xenograft model at a dose as low as 3 mg/kg. Its treatment delays U87-MG, MDA-MB-231 and OVCAR-3 xenograft growth. This chemical treatment demonstrates a safe toxicity profile in vivo. It selectively targets a wide variety of human cancer cell lines, as demonstrated by the in vitro data, while having little deleterious effects on normal cells[2].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 SHP-77 cells
濃度 100, 250, 1000 nM
反応時間 48 h
実験の流れ

SHP-77 cells were cultured with various concentrations of COTI-2 for 48 h. Cells were then washed twice with 1X cold PBS and stained with Annexin V and 7AAD. Briefly, 5 μl of Annexin V and 7AAD were added to 1 × 105 cells and incubated for 15 min at room temperature in the dark. Then 400 μl of the 1X binding buffer was added to the cells.
動物実験 動物モデル NCr-nu mice
投薬量 10 mg/kg
投与方法 i.p.

参考

  • https://www.nature.com/articles/nrc.2017.109
  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5173065/

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：

ABCC1 promotes GSH-dependent iron transport and resistance to Fe(II) and Cu(II) chelators [ Biometals, 2025, 10.1007/s10534-025-00736-z] PubMed: 40855238
The combination of breast cancer PDO and mini-PDX platform for drug screening and individualized treatment [ J Cell Mol Med, 2024, 28(9):e18374] PubMed: 38722288
Generation of an Isogenic Cell Line Model to Test Novel Treatment Options for TP53-Mutant AML [ DASH, 2020, None] PubMed: None

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。