CAS 186497-07-4|Zibotentan (ZD4054)

Introduction：Basic information about CAS 186497-07-4|Zibotentan (ZD4054), including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Zibotentan (ZD4054) BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Articles1
6. Synonyms

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	/
MSDS	ChineseUSA	Flash Point	339.0±34.3 °C
Symbol	GHS07	Signal Word	Warning

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) BiologicalActivity

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	Signaling Pathways >>GPCR/G Protein >>Endothelin ReceptorResearch Areas >>Cancer
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.

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

Signaling Pathways >>GPCR/G Protein >>Endothelin ReceptorResearch Areas >>Cancer

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

Articles1

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

Recommended......