1. Apoptosis
  2. Apoptosis

Elesclomol (Synonyms: STA-4783)

Cat. No.: HY-12040 Purity: 99.43%
Data Sheet SDS Handling Instructions

Elesclomol is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells.

For research use only. We do not sell to patients.
Elesclomol Chemical Structure

Elesclomol Chemical Structure

CAS No. : 488832-69-5

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10 mM * 1 mL in DMSO $110 In-stock
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10 mg $150 In-stock
50 mg $600 In-stock
100 mg $950 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Elesclomol is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells.

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) 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].

Clinical Trial
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References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.4968 mL 12.4838 mL 24.9675 mL
5 mM 0.4994 mL 2.4968 mL 4.9935 mL
10 mM 0.2497 mL 1.2484 mL 2.4968 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[3]

For viability assays, HBL and HBL-ρ0 cells are incubated with 300 nM elesclomol-Cu or Cu for 24 h. Cell death is determined using propidium iodide (5 µg/mL in PBS) staining and FACS analysis. Inner mitochondrial transmembrane potential is measured by incubating cells (25×104/mL) with 40 nM DIOC6(3) for 15 minutes at 37°C immediately prior to flow cytometry. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

400.52

Formula

C₁₉H₂₀N₄O₂S₂

CAS No.

488832-69-5

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 22 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.43%

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Elesclomol
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