| Cas No.: | 186497-07-4 |
| Synonyms: | ZD4054;ZD-4054;ZD 4054 |
| SMILES: | CC1=CN=C(C(=N1)OC)NS(=O)(=O)C2=C(N=CC=C2)C3=CC=C(C=C3)C4=NN=CO4 |
| Formula: | C19H16N6O4S |
| M.Wt: | 424.4331 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | Zibotentan (ZD4054) is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM).Zibotentan is capable of inhibiting or reducing the multitude of effects that are evoked by ET-1 activation of the ETA receptor and which promote tumor survival, growth and progression. Zibotentan (ZD4054) treatment produced significant inhibition of tumor growth in ovarian and breast xenografts. |
| Target: | IC50 value: 21 nM Target: ETA receptor |
| References: | [1]. Zibotentan James, N.D., Growcott, J.W. Drugs Fut 2009, 34(8): 624. [2]. Clarkson-Jones JA, Kenyon AS, Kemp J, Lenz EM, Oliver SD, Swaisland H.,Disposition and metabolism of the specific endothelin A receptor antagonist zibotentan (ZD4054) in healthy volunteers.,Xenobiotica. 2012 Apr;42(4):363-71. Epub 2011 Oct 20. [3]. Li J, Liu Y, Qian J, Wu L, Kemp J, Nii M, Tomkinson H, Zuo Y, Ranson M, Usami M.,Single- and multiple-dose pharmacokinetics, safety and tolerability of zibotentan (ZD4054) in Chinese men with advanced solid tumors.,Cancer Chemother Pharmacol. 2012 Jul;70( [4]. Nelson JB, Fizazi K, Miller K, Higano C, Moul JW, Akaza H, Morris T, McIntosh S, Pemberton K, Gleave M.,Phase 3, randomized, placebo-controlled study of zibotentan (ZD4054) in patients with castration-resistant prostate cancer metastatic to bone. ,Cancer [5]. Tomkinson H, Kemp J, Oliver S, Swaisland H, Taboada M, Morris T.,Pharmacokinetics and tolerability of zibotentan (ZD4054) in subjects with hepatic or renal impairment: two open-label comparative studies.,BMC Clin Pharmacol. 2011 Mar 17;11:3. |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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