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品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 5 mg/mL, clear (warmed)
儲存溫度
−20°C
SMILES 字串
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 密鑰
FJHHZXWJVIEFGJ-UHFFFAOYSA-N
基因資訊
human ... EDNRA(1909)
一般說明
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.
訊號詞
Warning
危險聲明
危險分類
Acute Tox. 4 Oral
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
A phase I study of zibotentan (ZD4054) in patients with metastatic, castrate-resistant prostate cancer.
Investigational New Drugs, 29(1), 118-125 (2011)
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