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Chemical Structure| 186497-07-4 Chemical Structure| 186497-07-4

Structure of Zibotentan
CAS No.: 186497-07-4

Chemical Structure| 186497-07-4

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Zibotentan is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM).

Synonyms: ZD4054

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Product Details of Zibotentan

CAS No. :186497-07-4
Formula : C19H16N6O4S
M.W : 424.43
SMILES Code : O=S(NC1=NC=C(C)N=C1OC)(C2=CC=CN=C2C3=CC=C(C4=NN=CO4)C=C3)=O
Synonyms :
ZD4054
MDL No. :MFCD09955343
InChI Key :FJHHZXWJVIEFGJ-UHFFFAOYSA-N
Pubchem ID :9910224

Safety of Zibotentan

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P301+P312+P330

Related Pathways of Zibotentan

GPCR

Isoform Comparison

Biological Activity

Target
  • ET-A

    ET-A, IC50:21 nM

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice Ovarian cancer metastasis model Intraperitoneal injection 10 mg/kg/day Once daily for 21 days To evaluate the inhibitory effect of ZD4054 on ovarian cancer metastasis PMC2650347
Wistar rats Aβ40-induced hypertension model Oral 3 mg/kg/d Once daily for 31 days Zibotentan abrogated the effects of Aβ40 infusion on baroreflex responsiveness and blood pressure, which declined, although without reduction in carotid blood flow, and Zibotentan caused uncoupling of the positive linear relationship between endothelin-1 and vascular endothelial growth factor, which as a sensor of tissue oxygenation would be expected to increase if there were hypoperfusion. PMC7081103
Wistar rats 4% salt-fed Wistar rats Oral 30, 100, 300 mg/kg/day Once daily for 7 or 14 days To evaluate the effect of Zibotentan on hematocrit and body weight, showing that Zibotentan dose-dependently reduced hematocrit and increased body weight, indicating fluid retention. PMC10539223

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00055471 - Completed - -
NCT00055471 Prostatic Neoplasms ... More >> Metastases, Neoplasm Less << Phase 2 Completed - United States, Ohio ... More >> Research Site Cleveland, Ohio, United States, 44195 United States, Wisconsin Research Site Madison, Wisconsin, United States Less <<
NCT00929162 Patients With Advanced Ovarian... More >> Cancer Sensitive to Platinum-based Chemotherapy Less << Phase 2 Terminated(Primary objective o... More >>f the trial was not met and so there was no benefit in collecting further information) Less << - Germany ... More >> Research Site Berlin, Germany Research Site Dresden, Germany Research Site Dusseldorf, Germany Research Site Essen, Germany Research Site Karlsruhe, Germany Research Site Kassel, Germany Research Site Kiel, Germany Research Site Lich, Germany Research Site Magdeburg, Germany Research Site Marburg, Germany Research Site Munchen, Germany Research Site Rostock, Germany Research Site Wiesbaden, Germany Italy Research Site Milano, MI, Italy Research Site Perugia, PG, Italy Research Site Aviano, PN, Italy Research Site Campobasso, Italy Research Site Modena, Italy Research Site Napoli, Italy Research Site Roma, Italy Less <<
NCT01000948 Prostate Cancer|Metastasis PHASE2 TERMINATED 2025-07-11 Dpt of Urology,Aarhus Universi... More >>ty Hospital, Aarhus, 8200, Denmark Less <<
NCT01205711 Colorectal Cancer Phase 2 Completed - United Kingdom ... More >> Leicester Royal Infirmary Leicester, England, United Kingdom, LE1 5WW Centre for Cancer Research and Cell Biology at Queen's University Belfast Belfast, Northern Ireland, United Kingdom, BT9 7AB Wales Cancer Trials Unit Cardiff, Wales, United Kingdom, CF11 9LJ Velindre Cancer Center at Velindre Hospital Cardiff, Wales, United Kingdom, CF14 2TL Less <<
NCT00929162 - Terminated(Primary objective o... More >>f the trial was not met and so there was no benefit in collecting further information) Less << - -
NCT01168141 Prostate Cancer|Metastasis UNKNOWN 2025-09-10 The Christie NHS Foundation Tr... More >>ust, Manchester, United Kingdom Less <<
NCT00314782 Prostate Cancer Phase 1 Completed - United States, New York ... More >> Research Site Buffalo, New York, United States United States, South Carolina Research Site Greenville, South Carolina, United States United States, Tennessee Research Site Nashville, Tennessee, United States Germany Research Site Berlin, Germany Research Site Dresden, Germany Research Site Rostock, Germany United Kingdom Research Site London, United Kingdom Research Site Plymouth, United Kingdom Research Site Surrey, United Kingdom Less <<
NCT01119118 Prostate Cancer PHASE2 TERMINATED 2025-11-11 University of Wisconsin Carbon... More >>e Cancer Center, Madison, Wisconsin, 53792, United States Less <<
NCT00745875 Non Small Cell Lung Cancer ... More >> Lung Cancer Less << Phase 2 Completed - Bulgaria ... More >> research Site Pleven, Bulgaria Research Site Sofia, Bulgaria Research Site Varna, Bulgaria Czech Republic Research Site Jicin, Czech Republic Research Site Prague, Czech Republic France Research Site Cedex, France Research Site Strasbourg, France Romania Research Site Bucharest, Romania Research Site Cluj-Napoca, Romania Ukraine Research Site Chernivtsi, Ukraine Research Site Kiev, Ukraine Research Site Sumy, Ukraine Research Site Uzngorod, Ukraine Less <<
NCT00745875 - Completed - -
NCT01119118 Prostate Cancer PHASE2 TERMINATED 2025-11-11 University of Wisconsin Carbon... More >>e Cancer Center, Madison, Wisconsin, 53792, United States Less <<
NCT00617669 - Completed - -
NCT02047708 Scleroderma|Scleroderma Renal ... More >>Crisis|Chronic Kidney Disease Less << PHASE2 COMPLETED 2025-10-17 Royal Free London NHS Foundati... More >>on Trust, London, NW32QG, United Kingdom Less <<
NCT01890135 Peripheral Arterial Disease ... More >> Intermittent Claudication Less << Phase 2 Completed - United States, Virginia ... More >> University Of Virginia Health System Charlottesville, Virginia, United States, 22908 Less <<
NCT00090363 Prostate Cancer Phase 2 Completed - -
NCT00617669 Prostate Cancer Phase 3 Completed - -
NCT00626548 Prostate Cancer Phase 3 Terminated(early efficacy revi... More >>ew by the Independent Data Monitoring Committee indicated it was unlikely to meet its primary efficacy endpoints) Less << - -
NCT00626548 - Terminated(early efficacy revi... More >>ew by the Independent Data Monitoring Committee indicated it was unlikely to meet its primary efficacy endpoints) Less << - -
NCT01134497 Metastatic Breast Cancer Phase 2 Withdrawn(New information on I... More >>MP affected the cost/benefit ratio) Less << - United Kingdom ... More >> Wales Cancer Trials Unit Cardiff, United Kingdom, CF14 4YS Less <<
NCT00554229 Prostate Cancer Phase 3 Completed - -
NCT00713336 Healthy Phase 1 Completed - United Kingdom ... More >> Research Site Macclesfield, United Kingdom Less <<
NCT00090363 - Completed - -
NCT00710047 Healthy Volunteers PHASE1 COMPLETED 2025-08-08 Research Site, Harrow, United ... More >>Kingdom Less <<
NCT00672581 Hepatic Impairment PHASE1 COMPLETED 2025-03-09 Research Site, Praha 4, Czech ... More >>Republic|Research Site, Praha 6, Czech Republic Less <<
NCT00713791 Healthy Phase 1 Completed - United States, Pennsylvania ... More >> Research Site Philadelphia, Pennsylvania, United States Less <<
NCT00709553 Healthy Phase 1 Completed - Germany ... More >> Research Site Berlin, Germany Less <<
NCT00997945 Advanced Solid Malignancies Phase 1 Completed - China, Shanghai ... More >> Research Site Shanghai, Shanghai, China Less <<
NCT00554229 - Completed - -
NCT06715670 Liver Cirrhosis PHASE1 RECRUITING 2025-03-03 Research Site, Glendale, Calif... More >>ornia, 91206, United States Less <<
NCT05112419 Hepatic Impairment|Renal Impai... More >>rment Less << PHASE1 COMPLETED 2021-12-15 Research Site, Sofia, 1612, Bu... More >>lgaria Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.36mL

0.47mL

0.24mL

11.78mL

2.36mL

1.18mL

23.56mL

4.71mL

2.36mL

References

 

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