Elesclomol (STA-4783)

製品コードS1052 バッチS105205

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.
Clear solution
5%DMSO 40%PEG300 5%Tween80 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。

 10.000mg/ml (24.97mM) Taking the 1 mL working solution as an example, add 50 μL of 200 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 make it clear; 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. 
* <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) is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells. Phase 3.Elesclomol specifically binds ferredoxin 1 (FDX1) α2/α3 helices and β5 strand and inhibits FDX1-mediated Fe-S cluster biosynthesis.Elesclomol (STA-4783) is a potent copper ionophore and can be used in the research of copper-dependent cell death (cuproptosis).
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. [1] 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. [2] 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. [3]
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. [4]

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
Tetrathiomolybdate alleviates bleomycin-induced pulmonary fibrosis by reducing copper concentration and suppressing EMT [ Eur J Med Res, 2025, 30(1):394] PubMed: 40390111
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
Copper-overload promotes ferroptosis in cervical cancer cells by upregulating HMOX1 expression [ Discov Oncol, 2025, 16(1):1549] PubMed: 40810778
MUC20 regulated by extrachromosomal circular DNA attenuates proteasome inhibitor resistance of multiple myeloma by modulating cuproptosis [ J Exp Clin Cancer Res, 2024, 43(1):68] PubMed: 38439082

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。

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