Zibotentan(Synonyms: ZD4054)

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Zibotentan (Synonyms: ZD4054) 纯度: 99.66%

Zibotentan (ZD4054) 是一种有效的，选择性的，具有口服活性的内皮素 A (ETA) 受体拮抗剂，Ki 为 13 nM。Zibotentan 对 ETB 没有抑制作用。Zibotentan 具有抗癌作用，可用于去势抵抗性前列腺癌 (CRPC) 的研究。

Zibotentan(Synonyms: ZD4054)

Zibotentan Chemical Structure

CAS No. : 186497-07-4

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10 mM * 1 mL in DMSO ￥1432 In-stock
5 mg ￥1302 In-stock
10 mg ￥2418 In-stock
50 mg ￥7440 In-stock
100 mg ￥9800 In-stock
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生物活性

Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a Ki of 13 nM. Zibotentan has no inhibitory effect on ETB. Zibotentan has anticancer effects and can be used for castration-resistant prostate cancer (CRPC) research[1][2].

IC50 & Target[1]

ETA

13 nM (Ki)

体外研究
(In Vitro)

Zibotentan potently inhibits the binding of 125iodine-ET-1 to cloned human ETA expressed in mouse erythroleukaemic cells, with a pIC50 (concentration to inhibit 50% of binding) value of 22 nM[1].
Zibotentan (48 hours) treatment increases the number of early apoptotic cells in serum-starved A2780 WT cells[2].
Zibotentan (ZD4054; 1 μM; 24 hours) treatment shows significant inhibition of cell proliferation in serum-starved HEY, OVCA 433, SKOV-3, and A-2780 cells[3].
Zibotentan (ZD4054; 1 μM; 48 hours) treatment induces an increase in apoptotic cells. Zibotentan inhibits bcl-2 and activates caspase-3 and poly(ADP-ribose) polymerase proteins.[3].
Zibotentan (ZD4054; 1 μM) decreases the endogenous ET-1-induced phosphorylation/activation of both kinases (AKT and p42/44MAPK) in HEY cells[3].
Zibotentan treatment also results in a reduction of ETAR-driven angiogenesis and invasive mediators, such as vascular endothelial growth factor, cyclooxygenase-1/2, and matrix metalloproteinase (MMP)[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[3]

Cell Line: HEY, OVCA 433, SKOV-3, and A-2780 cells
Concentration: 1 μM
Incubation Time: 24 hours
Result: Showed significant inhibition of cell proliferation.

Apoptosis Analysis[3]

Cell Line: HEY and OVCA 433 cells
Concentration: 1 μM
Incubation Time: 48 hours
Result: Induced an increase in apoptotic cells.

体内研究
(In Vivo)

Zibotentan (10 mg/kg; intraperitoneal injection; daily; for 21 days) treatment significantly inhibits tumor growth in mice. And Zibotentan treatment increases E-cadherin expression[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female athymic (nu+/nu+) mice (4-6 week of age) injected with wild-type A2780 cells[2]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; daily ; for 21 days
Result: Showed significant inhibition in tumor growth in mice.

Clinical Trial

分子量

424.43

Formula

C19H16N6O4S
CAS 号

186497-07-4
中文名称

齐泊腾坦；赛博特坦
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (58.90 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3561 mL 11.7805 mL 23.5610 mL
5 mM 0.4712 mL 2.3561 mL 4.7122 mL
10 mM 0.2356 mL 1.1781 mL 2.3561 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.89 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. C D Morris, et al. 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]. Laura Rosanò, et al. Acquisition of chemoresistance and EMT phenotype is linked with activation of the endothelin A receptor pathway in ovarian carcinoma cells. Clin Cancer Res. 2011 Apr 15;17(8):2350-60.

    [3]. Laura Rosanò, et al. 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.

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