Exemestane|107868-30-4|(依西美坦; FCE 24304; EXE)-陌孚医药/Medlife

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Exemestane (Synonyms: 依西美坦; FCE 24304; EXE)

目录号: PC10413 纯度: ≥98%

CAS No. :107868-30-4

商品编号	规格	价格	会员价
PC10413-10mg	10mg	¥637.00	请登录
PC10413-25mg	25mg	¥1337.00	请登录
PC10413-100mg	100mg	¥4204.00	请登录
PC10413-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥764.00	请登录

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中文名称

Exemestane

中文别名

依西美坦;依美司坦;1,4-二烯-3,17-二酮-6-亚甲基雄烷;6-亚甲基雄甾-1,4-二烯-3,17-二酮;伊西美坦;(8R,9S,10R,13S,14S)-6-亚甲基-10,13-二甲基-7,8,9,11,12,13,15,16-八氢-6H-环戊并[A]菲-3,17(10H,14H)-二酮;依西美坦(企标);依西美坦(甾体);3h咪唑并[4,5-b]吡啶-1-羧酸叔丁酯-2-酮;依西美坦标准品;依西美坦,In-house Standard;依西美坦-D3;依西美坦对照;依西美坦粉;依烯美坦;依西美坦(标准品);芳香酶(AROMATASE)抑制剂(EXEMESTANE)

英文名称

Exemestane

英文别名

6-Methylene-androsta-1,4-diene-3,17-dione;6-methylenandrosta-1,4-diene-3,17-dione;6-METHYLENEANDROSTA-1,4-DIENE-3,17-DIONE;10,13-dimethyl-6-methylidene-7,8,9,10,11,12,13,14,15,16-decahydrocyclopenta[a]phenanthrene-;EXEMESTANE;FCE-24304;AROMASIN;EXEMESTANCE;ExeMestane(AroMasin);Anti-Estrogen AI Exemestaneknightlabs_leeisun;6-methylenandrost-1,4-diene-3,17-dione;androsta-1,4-diene-6-methylene-3,17-dione;CE24304;EXALAMIDE;EXE;Exemestan;ExemestaneF;FCE 24304;PNU155971;ExeMestine;Exemestane D2;ExeMestane (USP);Exemestanum;Exemestano;Exemestanum [INN-Latin];Exemestano [INN-Spanish];Exemestane [USAN:INN:BAN];FCE24304;Aromasine;NY22HMQ4BX;1,4-Androstadien-3,17-dione-6-Methylene-d2;(8R,9S,10R,13S,14S)-10,13-Dimethyl-6-methylene-7,8,9,11,12,13,15,16-octahydro-6H-cyclopenta[a]phenanthrene-3,17(10H,14H)-dione;(8R,9S,10R,13S,14S)-10,13-diMethyl-6-Methylene-7,8,9,10,11,12,13,14,15,16-decahydro-3H-cyclopenta[a]phenanthrene-3,17(6H)-dione;ExeMestane SynonyMs 6-Methylenandrosta-1,4-diene-3,17-dione;6-Methylenandrosta-1,4-diene-3,17-dione;10,13-Dimethyl-6-methylidene-7,8,9,10,11,12,13,14,15,16-decahydrocyclopenta[a]phenanthrene-;Exemestance

Cas No.

107868-30-4

分子式

C₂₀H₂₄O₂

分子量

296.40

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC₅₀s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research.

性状

Solid

IC50 & Target[1][2]

Aromatase

体外研究(In Vitro)

Exemestane (EXE; 1-1000 nM; 72 hours; hFOB, Saos-2 cells<) treatment significantly increases the number of the cells.
Exemestane (0.1- μM; 72 hours) increases alkaline phosphatase activity in hFOB and Saos-2 cells and induces the expression of MYBL2, OSTM1, HOXD11, ADCYAP1R1, and glypican 2 in hFOB cells.
Exemestane competitively inhibits and time-dependently inactivates of human placental aromatase with K_i of 4.3 nM. Exemestane displaces [H]5α-dihydrotestosterone from rat prostate androgen receptor with IC₅₀ of 0.9 μM.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	hFOB, Saos-2 cells
Concentration:	1 nM, 10 nM, 100 nM, 1000 nM
Incubation Time:	72 hours
Result:	Induced cell proliferation.

体内研究(In Vivo)

Exemestane (EXE; 20-100 mg/kg; intramuscular injection; once weekly; for 16 weeks) treatment significantly increases the lumbar vertebral and femoral BMD, bending strength of the femur, compressive strength of the fifth lumbar vertebra, and trabecular bone volume. Exemestane significantly reduces an ovariectomy-induced increase in serum pyridinoline and serum osteocalcin. Exemestane causes significant reductions of serum cholesterol and low-density lipoprotein cholesterol.
Exemestane (20 mg/kg/day s.c.) induces 26% complete (CR) and 18% partial (PR) tumor regressions in rats with 7,12-dimethylbenzanthracene (DMBA)-induced mammary tumors.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female Sprague Dawley rats (10-month-old) bearing ovariectomy
Dosage:	20 mg/kg, 50 mg/kg, or 100 mg/kg
Administration:	Intramuscular injection; once weekly; for 16 weeks
Result:	Significantly increased the lumbar vertebral and femoral BMD, bending strength of the femur, compressive strength of the fifth lumbar vertebra, and trabecular bone volume.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. Di Salle, E., et al., Novel aromatase and 5 alpha-reductase inhibitors. J Steroid Biochem Mol Biol, 1994. 49(4-6): p. 289-94. [Information]

[2]. Miki, Y, et al. Effects of aromatase inhibitors on human osteoblast and osteoblast-like cells: a possible androgenic bone protective effects induced by exemestane. Bone. 2004 Sep 1;10(17):5717-23. [Information]

[3]. Goss, P.E., et al., Effects of the steroidal aromatase inhibitor exemestane and the nonsteroidal aromatase inhibitor letrozole on bone and lipid metabolism in ovariectomized rats. Clin Cancer Res, 2004. 10(17): p. 5717-23. [Information]

[4]. Zaccheo, T., D. Giudici, and E. Di Salle, Inhibitory effect of combined treatment with the aromatase inhibitor exemestane and tamoxifen on DMBA-induced mammary tumors in rats. J Steroid Biochem Mol Biol, 1993. 44(4-6): p. 677-80. [Information]

溶解度数据

体外研究:

DMSO : ≥ 54 mg/mL (182.19 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.3738 mL	16.8691 mL	33.7382 mL
5 mM	0.6748 mL	3.3738 mL	6.7476 mL
10 mM	0.3374 mL	1.6869 mL	3.3738 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (8.43 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.43 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (8.43 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.43 mM，饱和度未知) 的澄清溶液。
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 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.43 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.43 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。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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