Zibotentan (ZD4054)

Modify Date: 2025-08-20 18:13:15

Zibotentan (ZD4054) Structure
Zibotentan (ZD4054) structure
Common Name Zibotentan (ZD4054)
CAS Number 186497-07-4 Molecular Weight 424.433
Density 1.4±0.1 g/cm3 Boiling Point 637.0±65.0 °C at 760 mmHg
Molecular Formula C19H16N6O4S Melting Point N/A
MSDS Chinese USA Flash Point 339.0±34.3 °C
Symbol GHS07
GHS07
Signal Word Warning

 Use of Zibotentan (ZD4054)


Zibotentan (ZD4054) is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM). IC50 value: 21 nM Target: ETA receptorZibotentan 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.

 Names

Name N-(3-methoxy-5-methylpyrazin-2-yl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]pyridine-3-sulfonamide
Synonym More Synonyms

 Zibotentan (ZD4054) Biological Activity

Description Zibotentan (ZD4054) is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM). IC50 value: 21 nM Target: ETA receptorZibotentan 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.
Related Catalog
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.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Boiling Point 637.0±65.0 °C at 760 mmHg
Molecular Formula C19H16N6O4S
Molecular Weight 424.433
Flash Point 339.0±34.3 °C
Exact Mass 424.095367
PSA 141.37000
LogP 2.38
Vapour Pressure 0.0±1.9 mmHg at 25°C
Index of Refraction 1.628
InChIKey FJHHZXWJVIEFGJ-UHFFFAOYSA-N
SMILES COc1nc(C)cnc1NS(=O)(=O)c1cccnc1-c1ccc(-c2nnco2)cc1
Storage condition -20°C

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
Precautionary Statements P301 + P312 + P330
RIDADR NONH for all modes of transport
RTECS UT7937700

 Articles1

More Articles
A phase I study of zibotentan (ZD4054) in patients with metastatic, castrate-resistant prostate cancer. Schelman WR et al

Invest. New Drugs 29(1) , 118-25, (2011)

 Synonyms

N-(3-Methoxy-5-methyl-2-pyrazinyl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]-3-pyridinesulfonamide
Zd 4054
S1456_Selleck
ZD4054
Zibotentan
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