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Catalog: | HY-12040 |
Brand: | MCE |
CAS: | 488832-69-5 |
MDL | MFCD12911784 |
---|---|
Molecular Weight | 400.52 |
Molecular Formula | C19H20N4O2S2 |
SMILES | S=C(C1=CC=CC=C1)N(NC(CC(NN(C(C2=CC=CC=C2)=S)C)=O)=O)C |
Elesclomol (STA-4783) is a potent copper ionophore and promotes copper-dependent cell death ( cuproptosis ). Elesclomol specifically binds ferredoxin 1 (FDX1) α2/α3 helices and β5 strand. Elesclomol inhibits FDX1-mediated Fe-S cluster biosynthesis. Elesclomol is an oxidative stress inducer that induces cancer cell apoptosis . Elesclomol is a reactive oxygen species (ROS) inducer. Elesclomol can be used for Menkes and associated disorders of hereditary copper deficiency research [1] [2] [3] [4] .
Elesclomol (STA-4783) binds the FDX1 α2/α3 helices and β5 strand, but does not bind the paralog protein FDX2. Elesclomol-Cu(II) is an FDX1 neo-substrate. FDX1 protein binds and reduces the elesclomol-Cu(II) complex
[1]
.
Elesclomol-Cu (1:1 ratio) (40 nM) for only 2 hours results in a 15- to 60-fold increase in intracellular copper levels that triggered cell death more than 24 hours later in ABC1 cells
[1]
.
The addition of copper to elesclomol at a 1:1 molar ratio prior to treatment significantly reduces cell viability when cells are grown in glycolytic (glucose media) conditions
[2]
.
Elesclomol (200 nM; 18 hours) treatment increases the number of early and late apoptotic cells in HSB2 cells. Elesclomol induces apoptosis in cancer cells through the induction of oxidative stress
[3]
.
Elesclomol significantly inhibits the cell viability of SK-MEL-5, MCF-7, and HL-60 cells with IC
50
values of 110 nM, 24 nM and 9 nM, respectively
[5]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Apoptosis Analysis [3]
Cell Line: | HSB2 cells |
Concentration: | 200 nM |
Incubation Time: | 18 hours |
Result: | Increased the number of early and late apoptotic cells. |
Elesclomol (10 mg/kg; subcutaneous injection; every three days from post-natal day 5 to 26 and once weekly until post-natal day 54) treatment ameliorates severe cardiac pathology with a partial reduction in hypertrophy. Cardiac [Cu] increased with Elesclomol treatment from a vehicle knockout level of 34 to 55%
[4]
.
Elesclomol escorted copper to the mitochondria and increased cytochrome c oxidase levels in the brain. Elesclomol prevents detrimental neurodegenerative changes and improved the survival of the mottled-brindled mouse
[4]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: | Cardiac Ctr1 knockout mice [4] |
Dosage: | 10 mg/kg |
Administration: | Subcutaneous injection; every three days from post-natal day 5 to 26 and once weekly until post-natal day 54 |
Result: | Ameliorated severe cardiac pathology with a partial reduction in hypertrophy. |
NCT Number | Sponsor | Condition | Start Date | Phase |
---|---|---|---|---|
NCT00522834 | Synta Pharmaceuticals Corp. |
Melanoma
|
August 2007 | Phase 3 |
NCT00888615 | GOG Foundation|National Cancer Institute (NCI) |
Fallopian Tube Clear Cell Adenocarcinoma|Fallopian Tube Endometrioid Adenocarcinoma|Fallopian Tube Mucinous Adenocarcinoma|Fallopian Tube Serous Adenocarcinoma|Fallopian Tube Transitional Cell Carcinoma|Fallopian Tube Undifferentiated Carcinoma|Ovarian Brenner Tumor|Ovarian Clear Cell Adenocarcinoma|Ovarian Endometrioid Adenocarcinoma|Ovarian Mucinous Adenocarcinoma|Ovarian Seromucinous Carcinoma|Ovarian Serous Adenocarcinoma|Ovarian Transitional Cell Tumor|Ovarian Undifferentiated Carcinoma|Primary Peritoneal Serous Adenocarcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma
|
December 13, 2010 | Phase 2 |
NCT00808418 | Synta Pharmaceuticals Corp. |
Prostate Cancer
|
November 2008 | Phase 1 |
NCT00088088 | Synta Pharmaceuticals Corp. |
Stage IIIB Non-Small Cell Lung Cancer|Stage IV Non-Small Cell Lung Cancer
|
March 2004 | Phase 1|Phase 2 |
NCT00827203 | Synta Pharmaceuticals Corp. |
Metastatic Solid Tumors
|
January 2009 | Phase 1 |
NCT01280786 | Synta Pharmaceuticals Corp. |
Acute Myeloid Leukemia
|
January 2011 | Phase 1 |
NCT00084214 | Synta Pharmaceuticals Corp. |
Melanoma
|
May 2004 | Phase 1|Phase 2 |
NCT00087997 | Synta Pharmaceuticals Corp. |
Soft Tissue Sarcoma
|
July 2004 | Phase 2 |
Solid
Room temperature in continental US; may vary elsewhere.
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
DMSO : 100 mg/mL ( 249.68 mM ; Need ultrasonic)
Concentration Solvent 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 |
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