Elesclomol (STA-4783)

Description

Biological Activity

Protocol(Only for Reference)

Clinical Trial Information( data from http://clinicaltrials.gov)

Chemical Information

Cell Assay: ^[1]

Animal Study: ^[4]

References

貨號 Cat. No.: S1052
規格 Size: 5~200mg
品牌 Brand: Selleckchem

Elesclomol (STA-4783)

Catalog No.S1052

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

Size

Price

Stock

Quantity

10mM/1mLIn DMSO	USD 239	In stock	0 1 2 3 4 5 6 7 8 9 10
5mg	USD 214	In stock	0 1 2 3 4 5 6 7 8 9 10
10mg	USD 403	In stock	0 1 2 3 4 5 6 7 8 9 10
50mg	USD 1222	In stock	0 1 2 3 4 5 6 7 8 9 10
200mg	USD 3112	In stock	0 1 2 3 4 5 6 7 8 9 10

Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw

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 Models	Female CD-1 nude mice bearing established MDA435 breast cancer xenograft tumors
Dosages	~100 mg/kg
Administration	Intravenous injection
Solubility	1% DMSO/30% polyethylene glycol/1% Tween 80, 30 mg/mL

NCT Number	Recruitment	Conditions	Sponsor /Collaborators	Start Date	Phases
NCT00522834	Terminated	Melanoma	Synta Pharmaceuticals Corp.	2007-08	Phase 3
NCT00808418	Suspended	Prostate Cancer	Synta Pharmaceuticals Corp.	2008-11	Phase 1\|Phase 2
NCT00827203	Suspended	Metastatic Solid Tumors	Synta Pharmaceuticals Corp.	2009-01	Phase 1
NCT00888615	Suspended	Fallopian Tube Cancer\|Ovarian Cancer\|Primary Peritoneal Cavity Cancer	National Cancer Institute (NCI)\|Gynecologic Oncology Group	2010-12	Phase 2
NCT01280786	Recruiting	Acute Myeloid Leukemia	Synta Pharmaceuticals Corp.	2011-01	Phase 1

Description

Elesclomol (STA-4783) 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]

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]

Download Elesclomol (STA-4783) SDF

Molecular Weight (MW)	400.5
Formula	C₁₉H₂₀N₄O₂S₂
CAS No.	488832-69-5

Storage	3 years -20â„ƒPowder
Storage	6 months-80â„ƒin DMSO
Syonnyms	STA-4783

Solubility (25°C) *	In vitro	DMSO	80 mg/mL (199 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.