Estramustine phosphate sodium(Synonyms: 雌莫司汀磷酸钠)

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Estramustine phosphate sodium (Synonyms: 雌莫司汀磷酸钠) 纯度: 99.42%

Estramustine phosphate sodium,一种雌二醇类似物,是一种具有口服活性抗微管化疗剂。Estramustine phosphate sodium 通过与微管相关蛋白 (MAP) 和/或微管蛋白结合而使微管解聚。Estramustine phosphate sodium 可诱导前列腺癌细胞凋亡 (apoptosis),并可用于前列腺癌的研究。

Estramustine phosphate sodium(Synonyms: 雌莫司汀磷酸钠)

Estramustine phosphate sodium Chemical Structure

CAS No. : 52205-73-9

规格 价格 是否有货 数量
10 mM * 1 mL in Water ¥660 In-stock
10 mg ¥600 In-stock
50 mg ¥990 In-stock
100 mg ¥1400 In-stock
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生物活性

Estramustine phosphate sodium, an estradiol analog, is an orally active antimicrotubule chemotherapy agent. Estramustine phosphate sodium depolymerises microtubules by binding to microtubule associated proteins (MAPs) and/or to tubulin. Estramustine phosphate sodium induces prostate cancer cells apoptosis and can be used for prostate cancer research[1][2].

体外研究
(In Vitro)

Estramustine phosphate sodium (1 µg/mL) treatment suppressed PC3 cell growth[2].
Estramustine phosphate sodium (2 µg/mL) treatment significantly elevates phosphatidylserine eversion amount on PC3 cells. Estramustine phosphate sodium induces PC3 cell apoptosis[2].
Estramustine phosphate sodium (2 µg/mL) treatment decreases MiR-31 level. Estramustine phosphate odium induces s prostate cancer cell line PC3 apoptosis through reducing miR-31[2].
Estramustine phosphate sodium, a unique antitumour agent, is selectively taken up by prostate cells and exerts antineoplastic effects by interfering with microtubule of dynamics and by reducing plasma levels of testosterone[1].
Estrone and estradiol, products of the metabolism of Estramustine phosphate sodium, have shown antigonadotrophic activity resulting in reduced testosterone levels similar to those achieved after surgical castration[1].

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.

体内研究
(In Vivo)

Estramustine phosphate sodium (4-12 mg/kg; intraperitoneal injection; daily; for 2 weeks) inhibits PAC120 tumor growth 53% by day 35[4].

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: Swiss nu/nu (nude) male mice (5-week-old) bearing PAC120 tumors[3]
Dosage: 4 mg/kg, 12 mg/kg
Administration: Intraperitoneal injection; daily; for 2 weeks
Result: Suppressed the development of skin lesions and resulted in a dissociation between DTH response and antibody production.

Clinical Trial

分子量

564.35

Formula

C23H30Cl2NNa2O6P

CAS 号

52205-73-9

中文名称

雌莫司汀磷酸钠;雌莫司丁磷酸钠

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

H2O : 62.5 mg/mL (110.75 mM; Need ultrasonic)

DMSO : 5 mg/mL (8.86 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7720 mL 8.8598 mL 17.7195 mL
5 mM 0.3544 mL 1.7720 mL 3.5439 mL
10 mM 0.1772 mL 0.8860 mL 1.7720 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 (sealed storage, away from moisture and light)。-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: PBS

    Solubility: 65 mg/mL (115.18 mM); Clear solution; Need ultrasonic

*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]. Perry CM, et al. Estramustine phosphate sodium. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in prostate cancer. Drugs Aging. 1995 Jul;7(1):49-74.

    [2]. C Wei, et al. Estramustine phosphate induces prostate cancer cell line PC3 apoptosis by down-regulating miR-31 levels. Eur Rev Med Pharmacol Sci. 2018 Jan;22(1):40-45.

    [3]. Bergenheim AT, et al. Pharmacokinetics and pharmacodynamics of estramustine phosphate. Clin Pharmacokinet. 1998 Feb;34(2):163-72.

    [4]. Stephane Oudard, et al. Activity of docetaxel with or without estramustine phosphate versus mitoxantrone in androgen dependent and independent human prostate cancer xenografts. J Urol. 2003 May;169(5):1729-34.

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