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Merck
CN
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安全信息

SML1550

Sigma-Aldrich

Zibotentan

≥98% (HPLC)

别名:

N-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyridine-3-sulfonamide, ZD4054

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About This Item

经验公式（希尔记法）:
C19H16N6O4S
CAS号:
186497-07-4
分子量:
424.43
MDL编号:
MFCD09955343
UNSPSC代码:
12352200
PubChem化学物质编号:
329825958
NACRES:
NA.77

质量水平

100

检测方案

≥98% (HPLC)

形式

powder

颜色

white to beige

溶解性

DMSO: 5 mg/mL, clear (warmed)

储存温度

−20°C

SMILES字符串

O=S(C1=C(C2=CC=C(C3=NN=CO3)C=C2)N=CC=C1)(NC4=NC=C(C)N=C4OC)=O

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)

InChI key

FJHHZXWJVIEFGJ-UHFFFAOYSA-N

基因信息

human ... EDNRA(1909)

一般描述

Zibotentan is an orally bioavailable, non-peptide ETA (endothelin) receptor-specific antagonist, with no activity against ETB receptor.

生化/生理作用

Zibotentan has been found to inhibit cell proliferation, invasion and metastasis in cancer models. In clinical trials on patients with castration-resistant prostate cancer and bone metastasis, who were pain-free or had mild pain, zibotentan treatment resulted in better overall survival as compared to placebo.
Zibotentan is a potent and selective endothelin ET(A) receptor antagonist with an IC50 of 21 nM for the ETA receptor subtype and no binding observed even at 10,000 nM for ETB.

象形图

Exclamation mark
GHS07

警示用语：

Warning

危险声明

H302

危险分类

Acute Tox. 4 Oral

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

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A phase I study of zibotentan (ZD4054) in patients with metastatic, castrate-resistant prostate cancer.
Schelman WR et al
Investigational New Drugs, 29(1), 118-125 (2011)

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