Elesclomol (STA-4783)

製品コードS1052 バッチS105207

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）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
7.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 150 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. 
* <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 significantly induces the expression of heat shock stress response genes and metallothionein genes, a signature transcription profile indicative of oxidative stress in Hs294T cells. Elesclomol (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. Elesclomol 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] Elesclomol 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] Elesclomol induces copper-dependent ROS generation and cytoxicity in yeast. Instead of working through a specific cellular protein target, Elesclomol 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 (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), Elesclomol 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 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

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：

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
Protein phosphatase 1 regulatory subunit 15 A promotes translation initiation and induces G2M phase arrest during cuproptosis in cancers [ Cell Death Dis, 2024, 15(2):149] PubMed: 38365764
Systematic identification of anticancer drug targets reveals a nucleus-to-mitochondria ROS-sensing pathway [ Cell, 2023, 186(11):2361-2379.e25] PubMed: 37192619
Circulating extracellular vesicles are monitoring biomarkers of anti-PD1 response and enhancer of tumor progression and immunosuppression in metastatic melanoma [ J Exp Clin Cancer Res, 2023, 42(1):251] PubMed: 37759291
Metabolic modulation of mitochondrial mass during CD4+ T cell activation [ Cell Chem Biol, 2023, 30(9):1064-1075.e8] PubMed: 37716347
Integrated single-cell and bulk characterization of cuproptosis key regulator PDHB and association with tumor microenvironment infiltration in clear cell renal cell carcinoma [ Front Immunol, 2023, 14:1132661] PubMed: 37350959
Copper overload impairs hematopoietic stem and progenitor cell proliferation via prompting HSF1/SP1 aggregation and the subsequently downregulating FOXM1-Cytoskeleton axis [ iScience, 2023, 26(4):106406] PubMed: 37009226
ATF3/SPI1/SLC31A1 Signaling Promotes Cuproptosis Induced by Advanced Glycosylation End Products in Diabetic Myocardial Injury [ Int J Mol Sci, 2023, 24(2)1667] PubMed: 36675183
Perturbation of Copper Homeostasis Sensitizes Cancer Cells to Elevated Temperature [ Int J Mol Sci, 2023, 25(1)423] PubMed: 38203594
Identification of novel molecular subtypes and a signature to predict prognosis and therapeutic response based on cuproptosis-related genes in prostate cancer [ Front Oncol, 2023, 13:1162653] PubMed: 37205181

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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