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Chemical Structure| 488832-69-5 Chemical Structure| 488832-69-5

Structure of Elesclomol
CAS No.: 488832-69-5

Chemical Structure| 488832-69-5

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Elesclomol (STA-4783) is an effective copper ion carrier that promotes cuproptosis and acts as a reactive oxygen species (ROS) inducer, useful in the study of Menkes and related genetic copper deficiency disorders.

Synonyms: STA-4783

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Product Details of Elesclomol

CAS No. :488832-69-5
Formula : C19H20N4O2S2
M.W : 400.52
SMILES Code : O=C(NN(C)C(C1=CC=CC=C1)=S)CC(NN(C)C(C2=CC=CC=C2)=S)=O
Synonyms :
STA-4783
MDL No. :MFCD12911784
InChI Key :BKJIXTWSNXCKJH-UHFFFAOYSA-N
Pubchem ID :300471

Safety of Elesclomol

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Elesclomol

DNA

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
ATP7A KO B16 melanoma cell line 1 nM Partially rescued tyrosinase activity PMC7304446
Fibroblasts from a patient with SCO2 mutations 0.1 nM - 1 nM 3 or 6 days Partially rescued COX2 levels PMC6094114
Mouse embryonic fibroblasts (MEFs) 0.1 nM - 5 nM 3 days Rescued COX1 levels PMC6094114
Rat H9c2 cardiomyocytes 0.1 nM - 5 nM 3 days Rescued COX1 levels PMC6094114
Ctr1 knockout H9c2 rat cardiomyocytes 1 nM Restored oxygen consumption rate (OCR) and ATP levels, OCR restored to 103% of wild-type, ATP levels significantly increased PMC7304446
ABC1 cells 40 nM 2 h To investigate whether copper ionophore-mediated cell death is regulated, the results showed that short-term exposure to Elesclomol led to a significant increase in intracellular copper levels and triggered cell death more than 24 h later. PMC9273333
B16 mouse melanoma cells 0.4 μg/mL 24 h To evaluate the cytotoxicity of ES@CuO on B16 tumor cells, results showed that ES@CuO significantly inhibited tumor cell growth. PMC11095170
4T1 cells 74.75 nM 24 h To evaluate the antitumor activity of ECPCP on 4T1 cells, the results showed that ECPCP had an IC50 value of 74.75 nM, exhibiting the strongest cytotoxicity. PMC11187900
4T1 cells 100 nM, 1 μM 24 h Evaluate the antitumor activity of Elesclomol in 4T1 cells, results showed that Elesclomol significantly enhanced cytotoxicity in the presence of CuCl2, inducing Cu-dependent cell death. PMC11791997
QBC939 cells 10 nM 48 h To investigate the effect of Elesclomol and copper ion mixture (elesclomol-Cu) on cell death, results showed that elesclomol-Cu induced cell death, and the combination with ferroptosis inducers (such as sorafenib and erastin) enhanced cell death. PMC10242978
MHCC-97 H cells 10 nM 48 h To investigate the effect of Elesclomol and copper ion mixture (elesclomol-Cu) on cell death, results showed that elesclomol-Cu induced cell death, and the combination with ferroptosis inducers (such as sorafenib and erastin) enhanced cell death. PMC10242978
GSC-derived endothelial cells (GdECs) 10, 100, 1000 nM 48 h Elesclomol induced cell death in GdECs, increased mitochondrial reactive oxygen species (ROS) levels, leading to non-apoptotic copper-dependent cell death. PMC8273992
Glioblastoma stem-like cells (GSCs) 10, 100, 1000 nM 48 h Elesclomol induced cell death in GSCs, increased mitochondrial reactive oxygen species (ROS) levels, leading to non-apoptotic copper-dependent cell death. PMC8273992
HCT116 cells 0 to 100 μM 24 h To assess the impact of Elesclomol on cell viability, results showed the sensitivity of HCT116 cells to Elesclomol. PMC11663789
Yeast coa6Δ cells 0.8 nM Rescued respiratory growth defects by increasing mitochondrial copper content and restoring CcO activity PMC6094114

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Cardiac-specific Ctr1 KO mouse Subcutaneous injection 10 mg/kg Not specified ES treatment significantly improved survival rate, restored heart and spleen weights, partially reduced cardiac hypertrophy, and increased cardiac copper levels and COX1 levels PMC7304446
C57BL/6N mice B16 tumor model Intravenous injection 100 μg/mouse Every 2 days for a total of 3 times To evaluate the antitumor effect of ES@CuO in the B16 tumor model, results showed that ES@CuO significantly inhibited tumor growth. PMC11095170
Balb/c mice 4T1 tumor model Intravenous injection 5 mg/kg Every other day for four times To evaluate the antitumor efficacy of ECPCP in vivo, the results showed that ECPCP significantly inhibited tumor growth with an inhibition rate of 74.8%. PMC11187900
Nude mice MHCC-97 H and QBC939 xenograft model Intraperitoneal injection 40 mg/kg Five times a week, continuously monitored To investigate the inhibitory effect of Elesclomol and copper ion mixture (elesclomol-Cu) combined with sorafenib on hepatocellular carcinoma and intrahepatic cholangiocarcinoma in vivo, results showed that the combination significantly inhibited tumor growth. PMC10242978
NOD-SCID mice Glioblastoma xenograft model Intraperitoneal injection 25 mg/kg Three times per week for three weeks Elesclomol alone or in combination with temozolomide (TMZ) significantly inhibited tumor growth, and the combination therapy was more effective than TMZ alone. PMC8273992
Zebrafish Ctr1 mutant zebrafish Incubation in water 10 nM From 3 hpf onwards Rescued pigmentation defects and Cox1 levels PMC6094114
BALB/cAnN-Foxn1nu/nu/Rj nude mice 22Rv1 xenografts Intravenous injection 25–37 MBq Single or multiple doses, lasting 21 days Evaluate the therapeutic effects of [64Cu][Cu(ES)] in vivo, results showed [64Cu][Cu(ES)] significantly inhibited tumor growth PMC10547809

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00088088 Stage IIIB Non-Small Cell Lung... More >> Cancer Stage IV Non-Small Cell Lung Cancer Less << Phase 1 Phase 2 Completed - United States, Arkansas ... More >> NEA Clinic Jonesboro, Arkansas, United States, 72401 United States, California Wilshire Oncology Medical Group Pamona, California, United States, 91767 St. Francis Memorial Hospital San Francisco, California, United States Cancer Institute Medical Group Santa Monica, California, United States, 90404 Kaiser Permanete Vallejo, California, United States United States, Connecticut Oncology Associates of Bridgeport Trumball, Connecticut, United States, 06611 United States, Florida ACORN Miami, Florida, United States Oncology Hematology Consultants Sarasota, Florida, United States, 34236 United States, Illinois University of Chicago Chicago, Illinois, United States, 60637 The Cancer Institute at Alexian Brothers Elk Grove Village, Illinois, United States, 60007 Ingalls Hospital Harvey, Illinois, United States, 60426 United States, Louisiana Overton Brooks, VAMC Shreveport, Louisiana, United States, 71101 LSUHSC - Shreveport Feist Weiller Cancer Center Shreveport, Louisiana, United States, 71130 United States, Maryland Maryland Hematology and Oncology Associates Baltimore, Maryland, United States, 21236 United States, Minnesota The Duluth Clinic Duluth, Minnesota, United States, 55805 United States, Tennessee The West Clinic Memphis, Tennessee, United States, 38120 The Sarah Cannon Research Center Nashville, Tennessee, United States, 37203 United States, Texas Presbyterian Hospital Dallas, Texas, United States, 75231 United States, Washington Multicare Health System Tacoma, Washington, United States, 98405 Less <<
NCT00087997 Soft Tissue Sarcoma PHASE2 COMPLETED 2025-10-05 Arizona Cancer Center, Scottsd... More >>ale, Arizona, 85258, United States|Arizona Cancer Center, Tucson, Arizona, 85724, United States|UCLA, Los Angeles, California, 90095, United States|Yale University School of Medicine, New Haven, Connecticut, 06520, United States|University of Florida, Gainesville, Florida, 32610, United States|H. Lee Moffitt Cancer Center, Tampa, Florida, 33612, United States|Palm Beach Cancer Institute, West Palm Beach, Florida, 33401, United States|Winship Cancer Institute, Atlanta, Georgia, 30322, United States|University of Chicago Department of Medicine, Chicago, Illinois, 60637, United States|Via Christi Regional Med. Center (Wichita CCOP), Wichita, Kansas, 67214, United States|University of Louisville Hospital, Louisville, Kentucky, 40202, United States|Feist-Weiller Cancer Center, Shreveport, Louisiana, 71103, United States|Dana-Farber Cancer Institute, Boston, Massachusetts, 02115, United States|University of Michigan, Ann Arbor, Michigan, 48109, United States|Wayne State University, Detroit, Michigan, 48201, United States|Genesys Hurley Cancer Institute, Flint, Michigan, 48503, United States|Washington University School of Medicine, St. Louis, Missouri, 63110, United States|University of Nebraska Medical Center, Omaha, Nebraska, 68198, United States|NYU Cancer Institute Clinical Center, New York, New York, 10016, United States|Herbert Irving Cancer Center, New York, New York, 10032, United States|Carolinas Medical Center/Blumenthal Cancer Center, Charlotte, North Carolina, 28203, United States|Oregon Health and Science University, Portland, Oregon, 97239, United States|Hillman Cancer Center, Pittsburg, Pennsylvania, 15232, United States|The West Clinic, Memphis, Tennessee, 38120, United States|The Sarah Cannon Cancer Center, Nashville, Tennessee, 37203, United States|MD Anderson Cancer Center, Houston, Texas, 77030, United States|Mount Sinai Hospital, Toronto, Ontario, M5G 1X5, Canada Less <<
NCT00522834 Melanoma Phase 3 Terminated - -
NCT00088114 Neoplasms Phase 1 Completed - United States, Massachusetts ... More >> Beth Israel-Deaconess Medical Center Boston, Massachusetts, United States, 02215 Dana Farber Cancer Institute Boston, Massachusetts, United States, 02215 Less <<
NCT00827203 Metastatic Solid Tumors Phase 1 Suspended January 2011 United States, Maryland ... More >> Mayo Clinic Rochester, Maryland, United States, 55905 United States, Texas University of Texas Health Science Center, Cancer Therapy & Research Center, Institute for Drug Development San Antonio, Texas, United States, 78229 United States, Wisconsin University of Wisconsin Paul P. Carbone Comprehensive Cancer Center Madison, Wisconsin, United States, 53792 Less <<
NCT00888615 Fallopian Tube Clear Cell Aden... More >>ocarcinoma Fallopian Tube Endometrioid Adenocarcinoma Fallopian Tube Mucinous Adenocarcinoma Fallopian Tube Serous Adenocarcinoma Fallopian Tube Transitional Cell Carcinoma Ovarian Brenner Tumor Ovarian Clear Cell Adenocarcinoma Ovarian Endometrioid Adenocarcinoma Ovarian Mucinous Adenocarcinoma Ovarian Seromucinous Carcinoma Ovarian Serous Adenocarcinoma Ovarian Transitional Cell Tumor Primary Peritoneal Serous Adenocarcinoma Recurrent Fallopian Tube Carcinoma Recurrent Ovarian Carcinoma Recurrent Primary Peritoneal Carcinoma Undifferentiated Fallopian Tube Carcinoma Undifferentiated Ovarian Carcinoma Less << Phase 2 Active, not recruiting - -
NCT00084214 Melanoma Phase 1 Phase 2 Completed - -
NCT01280786 Acute Myeloid Leukemia Phase 1 Unknown August 2014 Canada, Ontario ... More >> Princess Margaret Hospital Toronto, Ontario, Canada, MSG 2M9 Less <<
NCT00808418 Prostate Cancer Phase 1 Completed - United States, California ... More >> Pacific Coast Hematology/Oncology Medical Group Fountain Valley, California, United States, 92708 United States, Maryland Mayo Clinic Rochester, Maryland, United States, 55905 United States, North Dakota Mid Dakota Clinic Bismarck, North Dakota, United States, 58501 United States, Texas University of Texas Health Science Center, Cancer Therapy & Research Center, Institute for Drug Development San Antonio, Texas, United States, 78229 United States, Wisconsin University of Wisconsin Paul P. Carbone Comprehensive Cancer Center Madison, Wisconsin, United States, 53792 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.50mL

0.50mL

0.25mL

12.48mL

2.50mL

1.25mL

24.97mL

4.99mL

2.50mL

References

 

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