Structure of Zibotentan
CAS No.: 186497-07-4
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Zibotentan is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM).
Synonyms: ZD4054
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Batch number can be found on the product's label following the word 'Batch'.
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Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
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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 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302 |
Precautionary Statements: | P301+P312+P330 |
Target |
|
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 << |
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 |
Tags: Zibotentan | ZD4054 | ZD 4054 | ZD-4054 | Endothelin Receptor | Apoptosis | 44MAPK | bcl-2 | caspase-3 | ETA receptor antagonist | endothelin A receptor | endothelin A | 186497-07-4
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P273 | Avoid release to the environment. |
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P281 | Use personal protective equipment as required. |
P282 | Wear cold insulating gloves/face shield/eye protection. |
P283 | Wear fire/flame resistant/retardant clothing. |
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P285 | In case of inadequate ventilation wear respiratory protection. |
P231 + P232 | Handle under inert gas. Protect from moisture. |
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Response | |
Code | Phrase |
P301 | IF SWALLOWED: |
P304 | IF INHALED: |
P305 | IF IN EYES: |
P306 | IF ON CLOTHING: |
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P310 | Immediately call a POISON CENTER or doctor/physician. |
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P312 | Call a POISON CENTER or doctor/physician if you feel unwell. |
P313 | Get medical advice/attention. |
P314 | Get medical advice/attention if you feel unwell. |
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P301 + P310 | IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician. |
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P302 + P334 | IF ON SKIN: Immerse in cool water/wrap in wet bandages. |
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P303 + P361 + P353 | IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower. |
P304 + P312 | IF INHALED: Call a POISON CENTER or doctor/physician if you feel unwell. |
P304 + P340 | IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing. |
P304 + P341 | IF INHALED: If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing. |
P305 + P351 + P338 | IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. |
P306 + P360 | IF ON CLOTHING: Rinse Immediately contaminated CLOTHING and SKIN with plenty of water before removing clothes. |
P307 + P311 | IF exposed: call a POISON CENTER or doctor/physician. |
P308 + P313 | IF exposed or concerned: Get medical advice/attention. |
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P332 + P313 | IF SKIN irritation occurs: Get medical advice/attention. |
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P335 + P334 | Brush off loose particles from skin. Immerse in cool water/wrap in wet bandages. |
P337 + P313 | IF eye irritation persists: Get medical advice/attention. |
P342 + P311 | IF experiencing respiratory symptoms: call a POISON CENTER or doctor/physician. |
P370 + P376 | In case of fire: Stop leak if safe to Do so. |
P370 + P378 | In case of fire: |
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P370 + P380 + P375 | In case of fire: Evacuate area. Fight fire remotely due to the risk of explosion. |
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H201 | Explosive; mass explosion hazard |
H202 | Explosive; severe projection hazard |
H203 | Explosive; fire, blast or projection hazard |
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H220 | Extremely flammable gas |
H221 | Flammable gas |
H222 | Extremely flammable aerosol |
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H231 | May react explosively even in the absence of air at elevated pressure and/or temperature |
H240 | Heating may cause an explosion |
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H242 | Heating may cause a fire |
H250 | Catches fire spontaneously if exposed to air |
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H260 | In contact with water releases flammable gases which may ignite spontaneously |
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H305 | May be harmful if swallowed and enters airways |
H310 | Fatal in contact with skin |
H311 | Toxic in contact with skin |
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H314 | Causes severe skin burns and eye damage |
H315 | Causes skin irritation |
H316 | Causes mild skin irritation |
H317 | May cause an allergic skin reaction |
H318 | Causes serious eye damage |
H319 | Causes serious eye irritation |
H320 | Causes eye irritation |
H330 | Fatal if inhaled |
H331 | Toxic if inhaled |
H332 | Harmful if inhaled |
H333 | May be harmful if inhaled |
H334 | May cause allergy or asthma symptoms or breathing difficulties if inhaled |
H335 | May cause respiratory irritation |
H336 | May cause drowsiness or dizziness |
H340 | May cause genetic defects |
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H351 | Suspected of causing cancer |
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H361d | Suspected of damaging the unborn child |
H362 | May cause harm to breast-fed children |
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H371 | May cause damage to organs |
H372 | Causes damage to organs through prolonged or repeated exposure |
H373 | May cause damage to organs through prolonged or repeated exposure |
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Code | Phrase |
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H411 | Toxic to aquatic life with long-lasting effects |
H412 | Harmful to aquatic life with long-lasting effects |
H413 | May cause long-lasting harmful effects to aquatic life |
H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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