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    Elesclomol (STA-4783)
    Elesclomol (STA-4783)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0876
    CAS #: 488832-69-5Purity ≥98%

    Description: Elesclomol (STA4783; STA-4783; STA4783) is a bis(thio-hydrazide amide)-based heat shock protein 70/HSP70 inducer as well as an oxidative stress inducer with potential antitumor and pro-apoptotic activity. It activates natural killer (NK) cell-mediated tumor killing and elicits pro-apoptosis events among tumor cells. It was developed by GSK company as a chemotherapy adjuvant but the trial was suspended due to safety concerns. 

    References: Mol Cancer Ther. 2008 Aug;7(8):2319-27; J Am Chem Soc. 2010 Apr 21;132(15):5469-78; Curr Opin Investig Drugs.2006 Jun;7(6):574-80.


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    Molecular Weight (MW)400.5
    FormulaC19H20N4O2S2
    CAS No.488832-69-5
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 80 mg/mL (199.8 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL
    Synonyms

    Synonym: STA 4783, Elesclomol; STA4783; STA-4783; 

    Chemical Name: N'1,N'3-dimethyl-N'1,N'3-di(phenylcarbonothioyl)malonohydrazide

    InChi Key: BKJIXTWSNXCKJH-UHFFFAOYSA-N

    InChi Code: InChI=1S/C19H20N4O2S2/c1-22(18(26)14-9-5-3-6-10-14)20-16(24)13-17(25)21-23(2)19(27)15-11-7-4-8-12-15/h3-12H,13H2,1-2H3,(H,20,24)(H,21,25)

    SMILES Code: O=C(NN(C)C(C1=CC=CC=C1)=S)CC(NN(C)C(C2=CC=CC=C2)=S)=O


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    In Vitro

    In vitro activity: 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. 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. 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.


    Cell Assay: 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.

    In VivoAlthough 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.
    Animal modelFemale CD-1 nude mice bearing established MDA435 breast cancer xenograft tumors
    Formulation & DosageDissolved in DMSO, and diluted in saline; 100 mg/kg; i.v. injection
    References

    Mol Cancer Ther. 2008 Aug;7(8):2319-27; J Am Chem Soc. 2010 Apr 21;132(15):5469-78; Curr Opin Investig Drugs. 2006 Jun;7(6):574-80.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Elesclomol (STA-4783)

    Elesclomol induces oxidative stress.



    Elesclomol (STA-4783)

    Elesclomol induces ROS and Hsp70 RNA at early times. Mol Cancer Ther. 2008 Aug;7(8):2319-27.
     

    Elesclomol (STA-4783)

    Elesclomol induces Hsp70 RNA via oxidative stress. Mol Cancer Ther. 2008 Aug;7(8):2319-27.
     

    Elesclomol (STA-4783)

    Oxidative stress mediates elesclomol-induced apoptosis. Mol Cancer Ther. 2008 Aug;7(8):2319-27.


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