Elesclomol (STA-4783)

Catalog No.S1052

Elesclomol (STA-4783) Chemical Structure

Molecular Weight(MW): 400.5

Elesclomol (STA-4783) is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells. Phase 3.

Size Price Stock Quantity  
In DMSO USD 190 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock

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2 Customer Reviews

  • 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.

    Oncotarget, 2016.. Elesclomol (STA-4783) purchased from Selleck.

    BMC Genomics 2014 15(1), 263. Elesclomol (STA-4783) purchased from Selleck.

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Biological Activity

Description Elesclomol (STA-4783) is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells. Phase 3.
Targets
HSP70 [1]
(Cell-free assay)
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 N-acetylcysteine (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 such as paclitaxel in these models, both in terms of tumor regression and extended survival of mice. [4]

Protocol

Cell Research:[1]
+ Expand
  • 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 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.
    (Only for Reference)
Animal Research:[4]
+ Expand
  • Animal Models: Female CD-1 nude mice bearing established MDA435 breast cancer xenograft tumors
  • Formulation: Dissolved in DMSO, and diluted in saline
  • Dosages: ~100 mg/kg
  • Administration: Intravenous injection
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 80 mg/mL (199.75 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 30 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.

Chemical Information

Molecular Weight 400.5
Formula

C19H20N4O2S2

CAS No. 488832-69-5
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01280786 Unknown status Acute Myeloid Leukemia Synta Pharmaceuticals Corp. January 2011 Phase 1
NCT00888615 Unknown status Malignant Ovarian Mixed Epithelial Tumor|Ovarian Brenner Tumor|Ovarian Clear Cell Cystadenocarcinoma|Ovarian Endometrioid Adenocarcinoma|Ovarian Mucinous Cystadenocarcinoma|Ovarian Serous Cystadenocarcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Undifferentiated Ovarian Carcinoma Gynecologic Oncology Group|National Cancer Institute (NCI) December 2010 Phase 2
NCT00827203 Suspended Metastatic Solid Tumors Synta Pharmaceuticals Corp. January 2009 Phase 1
NCT00808418 Completed Prostate Cancer Synta Pharmaceuticals Corp. November 2008 Phase 1
NCT00522834 Terminated Melanoma Synta Pharmaceuticals Corp. August 2007 Phase 3
NCT00087997 Completed Soft Tissue Sarcoma Synta Pharmaceuticals Corp. July 2004 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID