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Merck
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重要文件

SML1550

Sigma-Aldrich

Zibotentan

≥98% (HPLC)

同義詞:

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

經驗公式(希爾表示法):
C19H16N6O4S
CAS號碼:
分子量::
424.43
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77
暫時無法取得訂價和供貨情況

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.[1]

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.

象形圖

Exclamation mark

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


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分析證明 (COA)

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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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