For research use only. Not for therapeutic Use.
Zibotentan（Cat No.:I002404）, also known as ZD4054, is a selective antagonist of the endothelin A (ETA) receptor. It exhibits an inhibitory concentration 50 (IC50) of 21 nM against the ETA receptor, indicating its high affinity for this target. Notably, Zibotentan does not display inhibitory activity against the endothelin B (ETB) receptor. By specifically targeting the ETA receptor, Zibotentan has the potential to modulate endothelin signaling pathways and may be explored for therapeutic interventions in conditions involving dysregulation of ETA receptor-mediated processes.
| Catalog Number | I002404 |
| CAS Number | 186497-07-4 |
| Synonyms | N-(3-methoxy-5-methylpyrazin-2-yl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]pyridine-3-sulfonamide |
| Molecular Formula | C19H16N6O4S |
| Purity | ≥95% |
| Target | Endothelin Receptor |
| Solubility | DMSO ≥12mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL |
| Storage | -20°C |
| IC50 | 21 nM |
| IUPAC Name | N-(3-methoxy-5-methylpyrazin-2-yl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]pyridine-3-sulfonamide |
| InChI | InChI=1S/C19H16N6O4S/c1-12-10-21-17(19(23-12)28-2)25-30(26,27)15-4-3-9-20-16(15)13-5-7-14(8-6-13)18-24-22-11-29-18/h3-11H,1-2H3,(H,21,25) |
| InChIKey | FJHHZXWJVIEFGJ-UHFFFAOYSA-N |
| SMILES | CC1=CN=C(C(=N1)OC)NS(=O)(=O)C2=C(N=CC=C2)C3=CC=C(C=C3)C4=NN=CO4 |
| Reference | </br>1:The efficacy and safety of zibotentan in the treatment of castration-resistant prostate cancer: a meta-analysis. Wu Y, Shao N, Shen ZX, Li Q, Wang Y, Li C, Ma G, Dong J, Lu XJ, Feng NH.Eur Rev Med Pharmacol Sci. 2014;18(21):3291-6. Review. PMID: 25487941 Free Article</br>2:Efficacy of zibotentan in colorectal cancer–letter. Vlachostergios PJ.Mol Cancer Ther. 2014 Jun;13(6):1673. doi: 10.1158/1535-7163.MCT-13-0819. Epub 2014 May 16. No abstract available. PMID: 24837079 Free Article</br>3:Efficacy of zibotentan in colorectal cancer–response. Haque SU, Welch H, Dashwood M, Ramesh B, Loizidou M.Mol Cancer Ther. 2014 Jun;13(6):1674. doi: 10.1158/1535-7163.MCT-14-0002. Epub 2014 May 16. No abstract available. PMID: 24837078 Free Article</br>4:Efficacy of the specific endothelin a receptor antagonist zibotentan (ZD4054) in colorectal cancer: a preclinical study. Haque SU, Dashwood MR, Heetun M, Shiwen X, Farooqui N, Ramesh B, Welch H, Savage FJ, Ogunbiyi O, Abraham DJ, Loizidou M.Mol Cancer Ther. 2013 Aug;12(8):1556-67. doi: 10.1158/1535-7163.MCT-12-0975. Epub 2013 May 30. PMID: 23723122 Free Article</br>5:Phase III, randomized, placebo-controlled study of docetaxel in combination with zibotentan in patients with metastatic castration-resistant prostate cancer. Fizazi K, Higano CS, Nelson JB, Gleave M, Miller K, Morris T, Nathan FE, McIntosh S, Pemberton K, Moul JW.J Clin Oncol. 2013 May 10;31(14):1740-7. doi: 10.1200/JCO.2012.46.4149. Epub 2013 Apr 8. Erratum in: J Clin Oncol. 2014 Oct 20;32(30):3461. Fizazi, Karim S [Corrected to Fizazi, Karim]. PMID: 23569308 </br>6:Phase III, randomized, placebo-controlled study of once-daily oral zibotentan (ZD4054) in patients with non-metastatic castration-resistant prostate cancer. Miller K, Moul JW, Gleave M, Fizazi K, Nelson JB, Morris T, Nathan FE, McIntosh S, Pemberton K, Higano CS.Prostate Cancer Prostatic Dis. 2013 Jun;16(2):187-92. doi: 10.1038/pcan.2013.2. Epub 2013 Feb 5. PMID: 23381694 </br>7:A Phase II, randomized, double-blind study of zibotentan (ZD4054) in combination with carboplatin/paclitaxel versus placebo in combination with carboplatin/paclitaxel in patients with advanced ovarian cancer sensitive to platinum-based chemotherapy (AGO-OVAR 2.14). Cognetti F, Bagnato A, Colombo N, Savarese A, Scambia G, Sehouli J, Wimberger P, Sorio R, Harter P, Mari E, McIntosh S, Nathan F, Pemberton K, Baumann K.Gynecol Oncol. 2013 Jul;130(1):31-7. doi: 10.1016/j.ygyno.2012.12.004. Epub 2012 Dec 9. PMID: 23234805 </br>8:Phase 3, randomized, placebo-controlled study of zibotentan (ZD4054) in patients with castration-resistant prostate cancer metastatic to bone. Nelson JB, Fizazi K, Miller K, Higano C, Moul JW, Akaza H, Morris T, McIntosh S, Pemberton K, Gleave M.Cancer. 2012 Nov 15;118(22):5709-18. doi: 10.1002/cncr.27674. Epub 2012 Jul 11. PMID: 22786751 Free Article</br>9:Single- and multiple-dose pharmacokinetics, safety and tolerability of zibotentan (ZD4054) in Chinese men with advanced solid tumors. Li J, Liu Y, Qian J, Wu L, Kemp J, Nii M, Tomkinson H, Zuo Y, Ranson M, Usami M.Cancer Chemother Pharmacol. 2012 Jul;70(1):57-63. doi: 10.1007/s00280-012-1870-6. Epub 2012 May 22. PMID: 22618295 </br>10:Detection of previously unidentified metastatic disease as a leading cause of screening failure in a phase III trial of zibotentan versus placebo in patients with nonmetastatic, castration resistant prostate cancer. Yu EY, Miller K, Nelson J, Gleave M, Fizazi K, Moul JW, Nathan FE, Higano CS.J Urol. 2012 Jul;188(1):103-9. doi: 10.1016/j.juro.2012.03.008. Epub 2012 May 12. PMID: 22583636 Free PMC Article |
