Zibotentan (ZD4054)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
ZD4054是内皮素受体的特异性拮抗剂。
自分泌内皮素（ET）-1 /内皮素受体（ETAR）途径是参与卵巢癌发生的几个过程的重要调节器。
体外实验：在人卵巢癌ETAR阳性细胞系中，ZD4054有效抑制基底和ET-1诱导的细胞增殖，抑制AKT和p42 / 44 MAPK的磷酸化，并增加细胞凋亡，这是通过抑制bcl-2和活化caspase-3以及多聚（ADP-核糖）聚合酶蛋白发挥作用的[1]。
在体实验：在HEY卵巢癌异种移植中，ZD4054抑制肿瘤的生长，与紫杉醇抑制效果相当。ZD4054依赖性的肿瘤生长抑制与增殖指数、MMP-2表达和微血管密度的降低相关[2]。
临床试验：测定ZD4054在中国患者群体的PK和安全性情况，与先前报道类似。研究结果表明，在所分析的病人群体之间，ZD4054没有临床相关的种族间差异[3]。
参考文献：
[1] Morris CD, Rose A, Curwen J, Hughes AM, Wilson DJ, Webb DJ. Specific inhibition of the endothelin A receptor with ZD4054: clinical and pre-clinical evidence. Br J Cancer. 2005 Jun 20;92(12):2148-52.
[2] Rosanò L, Di Castro V, Spinella F, Nicotra MR, Natali PG, Bagnato A.ZD4054, a specific antagonist of the endothelin A receptor, inhibits tumor growth and enhances paclitaxel activity in human ovarian carcinoma in vitro and in vivo. Mol Cancer Ther. 2007 Jul;6(7):2003-11.
[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(1):57-63.
- 1. Qu L, Zhang X, et al. "Phenotypic assessment and ligand screening of ETA/ETB receptors with label-free dynamic mass redistribution assay." Naunyn Schmiedebergs Arch Pharmacol. 2019 Nov 28. PMID:31781785
- 2. Moody TW, Ramos-Alvarez I, et al. "Endothelin causes transactivation of the EGFR and HER2 in non-small cell lung cancer cells."j.peptides.2017.01.012. Epub 2017 Jan 31. PMID: 28153500
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 424.43 |
| Cas No. | 186497-07-4 |
| Formula | C19H16N6O4S |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥7.2 mg/mL in DMSO |
| Chemical Name | N-(3-methoxy-5-methylpyrazin-2-yl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]pyridine-3-sulfonamide |
| SDF | Download SDF |
| Canonical SMILES | CC1=CN=C(C(=N1)OC)NS(=O)(=O)C2=C(N=CC=C2)C3=CC=C(C=C3)C4=NN=CO4 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 描述 | Zibotentan（ZD4054）是内皮素（ET）A的特异性拮抗剂，IC50值为21 nM。 | |||||
| 靶点 | ETA | |||||
| IC50 | 21 nM | |||||
质量控制和MSDS
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化学结构
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