Estramustine is an antineoplastic agent. Estramustine depolymerizes microtnbules by binding to tubulin 1, exhibits antimitotic activity with an IC50 value of ~16 μM for mitosis of DU 145 cells. Estramustine blocks cells at mitosis in prostate tumor xenografts[1].
IC50 & Target
Tubulin 1[1]
分子量
440.40
Formula
C23H31Cl2NO3
CAS 号
2998-57-4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Dahllöf B, et al. Estramustine depolymerizes microtubules by binding to tubulin. Cancer Res. 1993 Oct 1;53(19):4573-81.
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:
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.