Elesclomol (STA-4783)

製品コードS1052 バッチS105203

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

C19H20N4O2S2
分子量 400.5 CAS No. 488832-69-5
Solubility (25°C)* 体外 DMSO 80 mg/mL (199.75 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 Elesclomol (STA-4783) は、腫瘍細胞間でアポトーシス促進イベントを誘発する新規の強力な酸化ストレス誘導剤です。 第3相。Elesclomolは、フェレドキシン1 (FDX1) のα2/α3ヘリックスおよびβ5ストランドに特異的に結合し、FDX1を介したFe-Sクラスター生合成を阻害します。Elesclomol (STA-4783) は強力な銅イオノフォアであり、銅依存性細胞死 (Cuproptosis) の研究に利用できます。
in vitro

Elesclomol (STA-4783) significantly induces the expression of heat shock stress response genes and metallothionein genes, a signature transcription profile indicative of oxidative stress in Hs294T cells. This compound (100 nM) rapidly induces Hsp70 RNA levels with a 4.8-fold increase at 1 hour and a 160-fold increase at 6 hours in Ramos Burkitt's lymphoma B cells in consistent with the intracellular ROS content which increases by 20% as early as 0.5 hour and 385% at 6 hours, and the induction of Hsp70 can be blocked by antioxidants NAC and Tiron pretreatment. It increases the number of early and late apoptotic cells with 3.7- and 11-fold through the induction of oxidative stress, which can be completely blocked by NAC, while having little effect on normal cells. The agent significantly inhibits the cell viability of SK-MEL-5, MCF-7, and HL-60 with IC50 of 110 nM, 24 nM and 9 nM, respectively. This chemical induces copper-dependent ROS generation and cytoxicity in yeast. Instead of working through a specific cellular protein target, it interacts with the electron transport chain (ETC), a biologically coherent set of processes occurring in the mitochondrion, to generate high levels of ROS within the organelle and consequently cell death.

in vivo

Although Elesclomol (STA-4783) (25-100 mg/kg) as a single agent shows no antitumor activity in nude mouse xenograft models of human breast cancers (MDA435, MCF7 and ZR-75-1), lung cancer (RER) or lymphoma (U937), this compound substantially enhances the efficacy of chemotherapeutic agents in these models, both in terms of tumor regression and extended survival of mice.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Hs294T, HSB2, and Ramos
濃度 Dissolved in DMSO at a concentration of 10 mM, final concentrations ~500 nM
反応時間 18, or 24 hours
実験の流れ

Cells are treated with various concentrations of Elesclomol (STA-4783) for 18 or 24 hours. The level of intracellular ROS is monitored using the DCFDA probe, which emits a green fluorescence on oxidation. Cell death is determined by flow cytometry of cells double stained with Annexin V/FITC and propidium iodide (PI) using a Vybrant Apoptosis assay kit.
動物実験 動物モデル Female CD-1 nude mice bearing established MDA435 breast cancer xenograft tumors
投薬量 ~100 mg/kg
投与方法 Intravenous injection

参考

  • https://pubmed.ncbi.nlm.nih.gov/18723479/
  • https://pubmed.ncbi.nlm.nih.gov/20345134/
  • https://pubmed.ncbi.nlm.nih.gov/22253786/
  • https://pubmed.ncbi.nlm.nih.gov/16784029/
  • https://pubmed.ncbi.nlm.nih.gov/35298263/

カスタマーフィードバック

Data from [BMC Genomics, 2014, 15(1), 263]

, , Oncotarget, 2016, 7(35):56933-56943

Data from [Data independently produced by , , Int J Biochem Cell Biol, 2017, 85:166-174]

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：

Mitochondrial-cytochrome c oxidase II promotes glutaminolysis to sustain tumor cell survival upon glucose deprivation [ Nat Commun, 2025, 16(1):212] PubMed: 39747079
PIK-III-Mediated Elevation of Thiamine Re-Sensitises Renal Cell Carcinoma to Cuproptosis via Activating PDHA1 [ Cell Prolif, 2025, e70101.] PubMed: 40741714
Prognostic models of immune-related cell death and stress unveil mechanisms driving macrophage phenotypic evolution in colorectal cancer [ J Transl Med, 2025, 23(1):127] PubMed: 39875913
UCHL3 augments cuproptosis via PKM2 deubiquitination in hepatocellular carcinoma [ Free Radic Biol Med, 2025, 237:65-75] PubMed: 40451468
p53 enhances elesclomol-Cu-induced cuproptosis in hepatocellular carcinoma via FDXR-mediated FDX1 upregulation [ Front Oncol, 2025, 15:1584811] PubMed: 40630211
CDC26 facilitates ferroptosis through SLC7A11 degradation and cell cycle arrest [ Clin Exp Med, 2025, 26(1):11] PubMed: 41249642
Tetrathiomolybdate alleviates bleomycin-induced pulmonary fibrosis by reducing copper concentration and suppressing EMT [ Eur J Med Res, 2025, 30(1):394] PubMed: 40390111
METTL14 promotes hippocampal neuronal cuproptosis via m6A modification on FDX1 mRNA in cerebral ischemia-reperfusion injury [ Brain Res Bull, 2025, 230:111504] PubMed: 40769372
Peripheral mitochondrial transplantation alleviates diabetes-associated cognitive dysfunction by suppressing cuproptosis [ Brain Res Bull, 2025, 222:111245] PubMed: 39924054
YTHDF3-associated m6A regulation and cuproptosis-related gene expression in steroid-induced osteonecrosis of the femoral head [ J Mol Histol, 2025, 56(5):279] PubMed: 40879675

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。