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依西美坦

依西美坦用途

Exemestane(FCE 24304)是芳香酶(aromatase)抑制剂,能抑制人胎盘和鼠卵巢芳香酶,IC50分别为30 nM和40 nM。

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依西美坦名称

[ CAS 号 ]:
107868-30-4

[ 中文名 ]:
依西美坦

[ 英文名 ]:
Exemestane

[中文别名 ]:

[英文别名 ]:

Exemestan
6-Methylenandrosta-1,4-diene-3,17-dione
6-methylenandrost-1,4-diene-3,17-dione
Aromasin
Exemestane
androsta-1,4-diene-6-methylene-3,17-dione
Exemestance
6-Methylene-androsta-1,4-diene-3,17-dione
MFCD00866994
6-Methyleneandrosta-1,4-diene-3,17-dione

依西美坦生物活性

[ 描述 ]:

Exemestane(FCE 24304)是芳香酶(aromatase)抑制剂,能抑制人胎盘和鼠卵巢芳香酶,IC50分别为30 nM和40 nM。

[ 相关类别 ]:

信号通路 >> 其他 >> 芳香

研究领域 >> 癌症

[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.

[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, 2007. 40(4): p. 876-87.

[3]. Wang, X. and S. Chen, Aromatase destabilizer: novel action of exemestane, a food and drug administration-approved aromatase inhibitor. Cancer Res, 2006. 66(21): p. 10281-6.

[4]. 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.

[5]. 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.

[相关活性小分子]

法倔唑 | N-去甲基-4-羟基-

依西美坦物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
453.7±45.0 °C at 760 mmHg

[ 熔点 ]:
155.13°C

[ 分子式 ]:
C₂₀H₂₄O₂

[ 分子量 ]:
296.403

[ 闪点 ]:
169.0±25.7 °C

[ 精确质量 ]:
296.177643

[ PSA ]:
34.14000

[ LogP ]:
3.11

[ 外观性状 ]:
白色至淡黄色晶体粉末

[ 蒸汽压 ]:
0.0±1.1 mmHg at 25°C

[ 折射率 ]:
1.572

[ 储存条件 ]:
Store at -20°C

依西美坦安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H319-H360

[ 警示性声明 ]:
P201-P305 + P351 + P338-P308 + P313

[ 危害码 (欧洲) ]:
T,N

[ 风险声明 (欧洲) ]:
60-61-51

[ 安全声明 (欧洲) ]:
S26-S36/37/39

[ 危险品运输编码 ]:
UN 3261 8/PG 2

[ WGK德国 ]:
3

[ 包装等级 ]:
III

[ 危险类别 ]:
8

[ 海关编码 ]:
2937900090

依西美坦合成路线

详细合成路线

依西美坦上下游产品

依西美坦上游产品

依西美坦下游产品

依西美坦制备

1.雄甾-4-烯-3，17-二酮和原甲酸三乙酯溶于四氢呋喃和无水乙醇中，在对甲苯磺酸存在下反应，然后加入N-甲基苯胺和甲醛溶液，继续反应。得到的Mannich反应产物溶于苯甲酸和无水二嚼烷，在DDQ作用下，得到依西美坦，总收率45%。

2.雄甾-4-烯-3,17-二酮和原甲酸三乙酯溶于四氢呋喃和无水乙醇中，在对甲苯磺酸存在下反应，然后加入犖-甲基苯胺和甲醛溶液，继续反应。得到的反应产物溶于苯甲酸和无水二烷，二氯二氰基苯醌(DDDQ)作用下，得到依西美坦。

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依西美坦海关

[ 海关编码 ]: 2937900090

[ 中文概述 ]:
HS: 2937900090 其他激素及其衍生物和结构类似物退税率:9.0% 监管条件:Q(进口药品通关单) 增值税率:17.0% 最惠国关税:4.0% 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 包装

[ 监管条件 ]: Q.进口药品通关单

[ Summary ]:
HS: 2937900090 Tax rebate rate:9.0% Supervision conditions:q(report of inspection of soundness on import medicines) VAT:17.0% MFN tariff:4.0% General tariff:30.0%

依西美坦文献

High throughput quantification of prohibited substances in plasma using thin film solid phase microextraction.

J. Chromatogr. A. 1374 , 40-9, (2014)

Simple, fast and efficient sample preparation approaches that allow high-throughput isolation of various compounds from complex matrices are highly desired in bioanalysis. Particularly sought are meth...

Synergistic effects of combined treatment with simvastatin and exemestane on MCF-7 human breast cancer cells.

Mol. Med. Report. 12 , 456-62, (2015)

Breast cancer is associated with high levels of incidence, morbidity and mortality; therefore, the identification of effective chemopreventive strategies is crucial. It is important for clinicians to ...

Adjuvant exemestane with ovarian suppression in premenopausal breast cancer.

N. Engl. J. Med. 371(2) , 107-18, (2014)

Adjuvant therapy with an aromatase inhibitor improves outcomes, as compared with tamoxifen, in postmenopausal women with hormone-receptor-positive breast cancer.In two phase 3 trials, we randomly assi...

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