Elesclomol (STA-4783)

Catalog No.S1052 Batch:S105204

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Technical Data

Formula

C19H20N4O2S2
Molecular Weight 400.5 CAS No. 488832-69-5
Solubility (25°C)* In vitro DMSO 80 mg/mL (199.75 mM)
Water Insoluble
Ethanol Insoluble
In Vivo (Add solvents to the product individually and in order.)
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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Elesclomol (STA-4783) is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumour 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).
Targets
HSP70
(Cell-free assay)
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 cytotoxicity 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 antitumour 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 tumour regression and extended survival of mice.

Protocol (from reference)

Cell Assay:

[1]
  • Cell Lines

    Hs294T, HSB2, and Ramos

  • Concentrations

    Dissolved in DMSO at a concentration of 10 mM, final concentrations ~500 nM

  • Incubation Time

    18, or 24 hours

  • Method

    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.
Animal Study:

[4]
  • Animal Models

    Female CD-1 nude mice bearing established MDA435 breast cancer xenograft tumors

  • Dosages

    ~100 mg/kg

  • Administration

    Intravenous injection

References

  • 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/

Customer Product Validation

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

<p>Treatment with elesclomol inhibits cancer cell growth and induces apoptosis by increasing ROS levels. a. Cell growth of SMOV2, IGROV1, and OVCA432 ovarian cancer cells treated with elesclomol in the presence or absence of the antioxidant NAC for 72 h. Cell growth was measured using the WST-1 assay and quantified relative to DMSO treated controls.</p>

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

Overexpression of GILZ favors oxidative cell death Dose-response of ROS production (HE staining) (A) or cell death (PI staining) (B) in indicated cells exposed toincreasing concentrations of elesclomol for 24 h (mean ± SD, n = 3, *p < 0.05). Alternatively, cells were treated with elesclomol for 24 h with or without pre-incubation with10 mM N-Acetyl Cysteine (NAC) for 12 h before HE staining (A) or PI staining (B) (mean ± SD, n = 3, *p < 0.05).

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

The proliferation of PC3 and LNCaP cells exposed to elesclomol at a range of concentrations for 48 h was assessed using MTT assay. Results are expressed as percentage of MTT absorbance of untreated cells at 0 h. p < .05 and p < .01 compared to untreated controls. Data are means ± SEM; n = 4.

Data from [ , , Int J Radiat Biol, 2017, 93(2):194-203 ]

Sellecks Elesclomol (STA-4783) Has Been Cited by 122 Publications

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
UCHL3 augments cuproptosis via PKM2 deubiquitination in hepatocellular carcinoma [ Free Radic Biol Med, 2025, 237:65-75] PubMed: 40451468
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
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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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