Elesclomol (STA-4783)

Catalog No.S1052

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

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Elesclomol (STA-4783) Chemical Structure

Elesclomol (STA-4783) Chemical Structure
Molecular Weight: 400.5

Validation & Quality Control

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Quality Control & MSDS

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Elesclomol (STA-4783) is available in the following compound libraries:

Product Information

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Product Description

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]
Features

Protocol(Only for 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 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
Formulation Dissolved in DMSO, and diluted in saline
Dosages ~100 mg/kg
Administration Intravenous injection

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Kirshner JR, et al. Mol Cancer Ther, 2008, 7(8), 2319-2327.

[2] Bair JS, et al. J Am Chem Soc, 2010, 132(15, 5469-5478.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-05-29)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01280786 Active, not recruiting Acute Myeloid Leukemia Synta Pharmaceuticals Corp. January 2011 Phase 1
NCT00888615 Recruiting Malignant Ovarian Mixed Epithelial Tumor|Ovarian Brenner Tumor|Ovarian Clear Cell Cystadenocarcinoma|Ovarian Endometrioid Adenocarcinoma|Ovarian Mu  ...more 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

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Chemical Information

Download Elesclomol (STA-4783) SDF
Molecular Weight (MW) 400.5
Formula

C19H20N4O2S2

CAS No. 488832-69-5
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 80 mg/mL (199.75 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
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 Name N1',N3'-dimethyl-N1',N3'-di(phenylcarbonothioyl)malonohydrazide

Customer Product Validation (1)


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Rating
Source BMC Genomics 2014 15(1), 263. Elesclomol (STA-4783) purchased from Selleck
Method Respiratory growth examination
Cell Lines yeast
Concentrations 0.228 uM
Incubation Time
Results Elesclomol conferred significant resistance to the copper chelating agent bathocuproine disulfonic acid disodium salt (BCS).

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