Elesclomol (STA-4783)

For research use only.

Catalog No.S1052

11 publications

Elesclomol (STA-4783) Chemical Structure

CAS No. 488832-69-5

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

Selleck's Elesclomol (STA-4783) has been cited by 11 publications

4 Customer Reviews

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

    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, 7(35):56933-56943. Elesclomol (STA-4783) purchased from Selleck.

  • 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).

    Int J Biochem Cell Biol, 2017, 85:166-174. Elesclomol (STA-4783) purchased from Selleck.

    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.

    Int J Radiat Biol, 2017, 93(2):194-203. Elesclomol (STA-4783) purchased from Selleck.

Purity & Quality Control

Choose Selective HSP (HSP90) Inhibitors

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PC3 cells M1naTGZ2dmO2aX;uJIF{e2G7 NFK4WHRKdmirYnn0bY9vKG:oIGDET|EudWWmaXH0[YQhSUuWIIDoc5NxcG:{eXzheIlwdiCjdDDUbJI{ODhicnXzbYR2\SCrbjDoeY1idiCSQ{OgZ4VtdHNiYomgSWxKW0FuIFnDOVA:OC5zMUOg{txO MlzVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|NEG2O|UoRjJzM{SxOlc2RC:jPh?=
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OCI-AML2 cells MnXqVJJwdGmoZYLheIlwdiCjc4PhfS=> MVLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE:FST3BUWwzKGOnbHzzMEBKSzVyPUCuN|Uh|ryP MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN2MU[3OUc,OjF|NEG2O|U9N2F-
K562 cells NEK5b2lRem:uaX\ldoF1cW:wIHHzd4F6 NVfCc5RnSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzMEBKSzVyPUG4JO69VQ>? MlOxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|NEG2O|UoRjJzM{SxOlc2RC:jPh?=
MES-SA MmjtR5l1d3SxeHnjbZR6KGG|c3H5 MYXDfZRwfG:6aXPpeJkh[WejaX7zeEBufWy2aXTyeYcuemW|aYP0ZY51KGi3bXHuJG1GWy2VQTDj[YxteyxiSVO1NF0xNjByNd88UU4> MnjUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{e5PFEoRjJ|OUO3PVgyRC:jPh?=
MES-SA/Dx5 MYfDfZRwfG:6aXPpeJkh[XO|YYm= M{LzPWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1GWy2VQT;EfFUh[2WubIOsJGlEPTB;MD6wNFXPxE1w M{HiSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUO3PVgyLz5{M{mzO|k5OTxxYU6=
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MES-SA M4TZZWN6fG:2b4jpZ4l1gSCjc4PhfS=> M1X4cmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1GWy2VQTDj[YxteyxiSVO1NF0xNjB3zszNMi=> M{LJO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUO3PVgyLz5{M{mzO|k5OTxxYU6=
MIP101 MV;DfZRwfG:6aXPpeJkh[XO|YYm= MXXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNTXAyODFiY3XscJMtKEmFNUC9NE4xPc7:TT6= NXXHSINpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5N|c6QDFpPkKzPVM4QThzPD;hQi=>
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Clone A MljtR5l1d3SxeHnjbZR6KGG|c3H5 M3XVcmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGNtd26nIFGgZ4VtdHNuIFnDOVA:OC5zzszNMi=> NYriRmpRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5N|c6QDFpPkKzPVM4QThzPD;hQi=>
Bowes MoHJR5l1d3SxeHnjbZR6KGG|c3H5 MUDDfZRwfG:6aXPpeJkh[WejaX7zeEB4cWymIIT5dIUhcHWvYX6gRo94\XNiY3XscJMtKEmFNUC9NE4z|ryPLh?= MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl|N{m4NUc,OjN7M{e5PFE9N2F-
HL60 MmLkR5l1d3SxeHnjbZR6KGG|c3H5 NXLXZmNQS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEx4MDDj[YxteyxiSVO1NF0xNjUQvF2u NF:4S5g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{mzO|k5OSd-MkO5N|c6QDF:L3G+
MDA435 MUHDfZRwfG:6aXPpeJkh[XO|YYm= MlTrR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCPDN3IHPlcIx{NCCLQ{WwQVXPxE1w NEPPeFk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{mzO|k5OSd-MkO5N|c6QDF:L3G+
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... Click to View More Cell Line Experimental Data

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]
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  • 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]
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  • Animal Models: Female CD-1 nude mice bearing established MDA435 breast cancer xenograft tumors
  • Dosages: ~100 mg/kg
  • Administration: Intravenous injection
    (Only for Reference)

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(Data is from Selleck tests instead of citations):
5% DMSO+40%PEG300+5%Tween80 +50%H2O
For best results, use promptly after mixing.
10mg/mL

* 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
Smiles CN(C(=S)C1=CC=CC=C1)NC(=O)CC(=O)NN(C)C(=S)C2=CC=CC=C2

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00827203 Suspended Drug: Elesclomol Sodium Metastatic Solid Tumors Synta Pharmaceuticals Corp. January 2009 Phase 1
NCT00808418 Completed Drug: Elesclomol Sodium|Drug: Docetaxel Prostate Cancer Synta Pharmaceuticals Corp. November 2008 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    How can we use the compound for in vivo mouse studies?

  • Answer:

    S1052 in 1% DMSO+30% polyethylene glycol+1% Tween 80 is a suspension, it is fine for oral administration. You can also dissolve S1052 in 0.5-1% CMC-Na solution and treat the mice by oral gavage.

HSP (HSP90) Signaling Pathway Map

Related HSP (HSP90) Products

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID