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质量水平
方案
≥98% (HPLC)
表单
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.
Zibotentan is a potent and selective endothelin ET(A) receptor antagonist.
警示用语：
Warning
危险声明
危险分类
Acute Tox. 4 Oral
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
历史批次信息供参考:
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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