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来曲唑

来曲唑用途

Letrozole是芳香酶抑制剂,其 IC50 为1-13 nM。

来曲唑名称

[ CAS 号 ]:
112809-51-5

[ 中文名 ]:
来曲唑

[ 英文名 ]:
Letrozole

[中文别名 ]:

1-[双(4-氰基苯基)甲基]-1,2,4-三氮唑

[英文别名 ]:

UNII-7LKK855W8I
Letrozol
Letoval
5-[Bis(4-methylphenyl)methyl]-1H-1,2,4-triazole
1H-1,2,4-Triazole, 5-[bis(4-methylphenyl)methyl]-
Femera
MFCD00866241
[14C]-Letrozole
Femara
Letrozole

来曲唑生物活性

[ 描述 ]:

Letrozole是芳香酶抑制剂,其 IC50 为1-13 nM。

[ 相关类别 ]:

信号通路 >> 其他 >> 芳香

信号通路 >> 自噬 >> 自噬

研究领域 >> 癌症

[参考文献]

[1]. Haynes, B.P., et al., The pharmacology of letrozole. J Steroid Biochem Mol Biol, 2003. 87(1): p. 35-45.

[2]. Bhatnagar, A.S., et al., Highly selective inhibition of estrogen biosynthesis by CGS 20267, a new non-steroidal aromatase inhibitor. J Steroid Biochem Mol Biol, 1990. 37(6): p. 1021-7.

[3]. Dellapasqua, S. and M. Colleoni, Letrozole. Expert Opin Drug Metab Toxicol, 2010. 6(2): p. 251-9.

[4]. Lee, K., et al., An in vivo model of intratumoural aromatase using aromatase-transfected MCF7 human breast cancer cells. Int J Cancer, 1995. 62(3): p. 297-302.

[相关活性小分子]

法倔唑 | 依西美坦 | N-去甲基-4-羟基-

来曲唑物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
472.0±55.0 °C at 760 mmHg

[ 熔点 ]:
181-183ºC

[ 分子式 ]:
C₁₇H₁₁N₅

[ 分子量 ]:
263.337

[ 闪点 ]:
214.2±24.5 °C

[ 精确质量 ]:
263.142242

[ PSA ]:
78.29000

[ LogP ]:
3.70

[ 外观性状 ]:
白色至灰白色结晶粉末

[ 蒸汽压 ]:
0.0±1.2 mmHg at 25°C

[ 折射率 ]:
1.615

[ 储存条件 ]:
-20°C Freezer

来曲唑MSDS

来曲唑安全信息

[ 危害码 (欧洲) ]:
Xi: Irritant;C: Corrosive;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
26-36

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
DI4957000

[ 海关编码 ]:
2933990090

来曲唑合成路线

来曲唑上下游产品

来曲唑上游产品

来曲唑下游产品

来曲唑制备

【方法一】
4-溴甲基苯腈(I)和三唑在氯仿-乙腈中反应，生成物(Ⅱ)再和4-氟苯腈，在叔丁醇钾存在下，在二甲基甲酰胺中反应，即得来曲唑。

来曲唑海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

来曲唑文献

Comparison of tamoxifen and letrozole response in mammary preneoplasia of ER and aromatase overexpressing mice defines an immune-associated gene signature linked to tamoxifen resistance.

Carcinogenesis 36(1) , 122-32, (2015)

Response to breast cancer chemoprevention can depend upon host genetic makeup and initiating events leading up to preneoplasia. Increased expression of aromatase and estrogen receptor (ER) is found in...

Hypogonadism Associated with Cyp19a1 (Aromatase) Posttranscriptional Upregulation in Celf1 Knockout Mice.

Mol. Cell. Biol. 35 , 3244-53, (2015)

CELF1 is a multifunctional RNA-binding protein that controls several aspects of RNA fate. The targeted disruption of the Celf1 gene in mice causes male infertility due to impaired spermiogenesis, the ...

Aromatase (Cyp19a1b) in the pituitary is dynamically involved in the upregulation of lhb but not fshb in the vitellogenic female ricefield eel Monopterus albus.

Endocrinology 155(11) , 4531-41, (2014)

Aromatase, encoded by Cyp19a1, is expressed in the pituitary of vertebrates; however, its physiological relevance remains poorly defined. In teleosts, the duplicated cyp19a1b is preferentially express...

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来曲唑