Letrozole|CGS 20267|Aromatase|for research only|Ambeed

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Letrozole/来曲唑 {[allProObj[0].p_purity_real_show]}

货号：A278180 同义名： CGS 20267

Letrozole是一种非甾体芳香化酶抑制剂，高选择性抑制雄烯二酮/睾酮向雌二醇转化（Ki=11.5 nM），降低循环雌激素95%以上。通过解除雌激素对下丘脑负反馈，增加GnRH脉冲频率，用于绝经后ER+乳腺癌。

Letrozole/来曲唑化学结构
CAS号：112809-51-5

Letrozole/来曲唑 3D分子结构
CAS号：112809-51-5

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Letrozole/来曲唑纯度/质量文件产品仅供科研

货号：A278180 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]; • Nat. Electron., 2025, 8, 66-74. Ambeed. [ A100095 ]; • Adv. Mater., 2025, 2416621. Ambeed. [ A255324 , A420052 ]; • Adv. Mater., 2025, 2410493. Ambeed. [ A838608 ]; • Adv. Mater., 2025, 2420319. Ambeed. [ A106129 ]; 更多 >

芳香酶亚型比较

产品名称	Aromatase ↓ ↑	其他靶点	纯度
Exemestane	+++ Aromatase (human), IC50: 30 nM Aromatase (rat), IC50: 40 nM		97%
Letrozole			95%
Anastrozole	+++ Aromatase, IC50: 15 nM		97%
Obacunone	+ Aromatase, IC50: 28.4 μM	Nrf2	98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Letrozole/来曲唑生物活性

靶点	Aromatase Aromatase, IC50:0.07 nM-20 nM
描述	Aromatase has a key role in development and reproduction, it converts androgens to estrogens. In humans, aromatase is expressed in the granulosa cells of the ovarian follicle, the syncytiotrophoblasts of the placenta during pregnancy, and in the Leydig cells of testes^[6]. Letrozole is an aromatase inhibitor with IC50 value of 0.89 nM in JEG-3 cells. In various human glioma cell lines, including LN229, T98G, U373MG, U251MG, U87MG, letrozole inhibited aromatase with IC50 values ranging in 1.12 - 1.89 μM and cell proliferation with IC50 values ranging in 0.91 - 4.39 μM. In vivo, treatment with letrozole on the dose of 4 mg/kg once a day for 8 days exhibited a marked reduction of active tumor volume in Sprague-Dawley rats orthotopically implanted with C6 gliomas^[7]. In addition, administration of 10 μg/kg letrozole for 35 days reduced tumor growth in the intratumoral aromatase mouse model^[8]. Letrozole entered clinical trials on the basis of its high potency and selectivity for aromatase, the demonstration of unsurpassed anti-tumor effects in models of human breast cancer. Daily doses of 0.1 – 5 mg letrozole have been shown to suppress estradiol, estrone, and estrone sulfate plasma concentrations by 75 – 95% from baseline^[9].
作用机制	Letrozole inhibits the enzyme activity of intracellular aromatase and effectively blocking estrogen synthesis^[9].

Letrozole/来曲唑细胞研究

细胞系	浓度	检测类型	检测时间	活性说明	数据源
human BT549 cells		Growth inhibition assay	48 h	Growth inhibition of human BT549 cells after 48 hrs by sulforhodamine B assay, GI50=0.89 μM	20950898
human IGROV1 cells		Growth inhibition assay	48 h	Growth inhibition of human IGROV1 cells after 48 hrs by sulforhodamine B assay, GI50=0.095 μM	20950898
human JEG3 cells		Function assay		Inhibition of aromatase activity in human JEG3 cells, IC50=0.00089 μM	18590272
human MCF7 cells		Cytotoxicity assay	72 h	Cytotoxicity against estrogen-dependent human MCF7 cells after 72 hrs by MTT assay, IC50=0.007 μM	24345481

Letrozole/来曲唑动物研究

Dose

Rat: 0.002 mg/kg - 0.02 mg/kg^[3] (p.o.), 1 mg/kg^[4] (p.o.)

Administration

p.o.

Pharmacokinetics

Animal	Mice^[5]	Rats^[5]	Dogs^[5]
Dose	6 mg/kg	3 mg/kg	3 mg/kg
Administration	p.o.	p.o.	p.o.
C_max	10.7 - 11.4 μmol/L	5.1 - 10.0 μmol/L	12.1 - 15.5 μmol/L
T_1/2		36 - 38 h
AUC_0→24h		174 - 295 μmol·h/L	297 - 372 μmol·h/L

Letrozole/来曲唑参考文献

[1]Haynes BP, Dowsett M, et al. The pharmacology of letrozole. J Steroid Biochem Mol Biol. 2003 Oct;87(1):35-45.

[2]Bhatnagar AS, Hausler A, et al. Highly selective inhibition of estrogen biosynthesis by CGS 20267, a new non-steroidal aromatase inhibitor. J Steroid Biochem Mol Biol. 1990 Dec 20;37(6):1021-7.

[3]Kafali H, Iriadam M, et al. A novel tocolytic agent: effects of letrozole on gestational length and parturition time. Am J Perinatol. 2007 May;24(5):323-6. Epub 2007 May 21.

[4]Kakadia N, Patel P, et al. Effect of Vitex negundo L. seeds in letrozole induced polycystic ovarian syndrome. J Tradit Complement Med. 2018 Oct 11;9(4):336-345.

[5]Letrozole

[6]Brodie A, Njar V, Macedo LF, Vasaitis TS, Sabnis G. The Coffey Lecture: steroidogenic enzyme inhibitors and hormone dependent cancer. Urol Oncol. 2009 Jan-Feb;27(1):53-63.

[7]Dave N, Chow LM, Gudelsky GA, LaSance K, Qi X, Desai PB. Preclinical pharmacological evaluation of letrozole as a novel treatment for gliomas. Mol Cancer Ther. 2015 Apr;14(4):857-64.

[8]Brodie A, Lu Q, Liu Y, Long B. Aromatase inhibitors and their antitumor effects in model systems. Endocr Relat Cancer. 1999 Jun;6(2):205-10.

[9]Bhatnagar AS. The discovery and mechanism of action of letrozole. Breast Cancer Res Treat. 2007;105 Suppl 1(Suppl 1):7-17.

Letrozole/来曲唑实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.51mL

0.70mL

0.35mL

17.53mL

3.51mL

1.75mL

35.05mL

7.01mL

3.51mL

Letrozole/来曲唑技术信息

CAS号	112809-51-5
分子式	C₁₇H₁₁N₅
分子量	285.3
SMILES Code	N#CC1=CC=C(C(N2C=NC=N2)C3=CC=C(C#N)C=C3)C=C1
MDL No.	MFCD00866241

别名	CGS 20267
运输	蓝冰
InChI Key	HPJKCIUCZWXJDR-UHFFFAOYSA-N
Pubchem ID	3902

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, 2-8°C

溶解方案

细胞实验：

DMSO: 50 mg/mL(175.25 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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

方案一

方案二

动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 4.2 mg/mL clear

PO 0.5% CMC-Na 50 mg/mL suspension

细胞研究

细胞系	浓度	检测类型	检测时间	活性说明	数据源

human BT549 cells	Growth inhibition assay	48 h	Growth inhibition of human BT549 cells after 48 hrs by sulforhodamine B assay, GI50=0.89 μM	20950898
human IGROV1 cells	Growth inhibition assay	48 h	Growth inhibition of human IGROV1 cells after 48 hrs by sulforhodamine B assay, GI50=0.095 μM	20950898
human JEG3 cells	Function assay		Inhibition of aromatase activity in human JEG3 cells, IC50=0.00089 μM	18590272
human MCF7 cells	Cytotoxicity assay	72 h	Cytotoxicity against estrogen-dependent human MCF7 cells after 72 hrs by MTT assay, IC50=0.007 μM	24345481
human MCF7 cells	Growth inhibition assay	48 h	Growth inhibition of human MCF7 cells after 48 hrs by sulforhodamine B assay, GI50=0.7 μM	20950898
human MCF7a cells	Cytotoxicity assay		Cytotoxicity against human MCF7a cells expressing Tet-off-3betaHSD1-Arom assessed as inhibition of TST-stimulated cell proliferation measured after 10 days, EC50=4e-06 μM	22951074
human MDA-MB-231 cells	Growth inhibition assay	48 h	Growth inhibition of human MDA-MB-231 cells after 48 hrs by sulforhodamine B assay, GI50=0.15 μM	20950898
human MDA-MB-435 cells	Growth inhibition assay	48 h	Growth inhibition of human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay, GI50=0.067 μM	20950898
human MDA-N cells	Growth inhibition assay	48 h	Growth inhibition of human MDA-N cells after 48 hrs by sulforhodamine B assay, GI50=1.61 μM	20950898
human NCI/ADR-RES cells	Growth inhibition assay	48 h	Growth inhibition of human NCI/ADR-RES cells after 48 hrs by sulforhodamine B assay, GI50=1.16 μM	20950898
human OVCAR4 cells	Growth inhibition assay	48 h	Growth inhibition of human OVCAR4 cells after 48 hrs by sulforhodamine B assay, GI50=0.88 μM	20950898
human OVCAR5 cells	Growth inhibition assay	48 h	Growth inhibition of human OVCAR5 cells after 48 hrs by sulforhodamine B assay, GI50=1.62 μM	20950898
human OVCAR8 cells	Growth inhibition assay	48 h	Growth inhibition of human OVCAR8 cells after 48 hrs by sulforhodamine B assay, GI50=4.5 μM	20950898
human SKOV3 cells	Growth inhibition assay	48 h	Growth inhibition of human SKOV3 cells after 48 hrs by sulforhodamine B assay, GI50=1.09 μM	20950898
human T47D cells	Growth inhibition assay	48 h	Growth inhibition of human T47D cells after 48 hrs by sulforhodamine B assay, GI50=0.44 μM	20950898

Letrozole/来曲唑 {[allProObj[0].p_purity_real_show]}

Letrozole/来曲唑纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Letrozole/来曲唑质控信息

Letrozole/来曲唑生物活性

Letrozole/来曲唑细胞研究

Letrozole/来曲唑动物研究

Letrozole/来曲唑参考文献

Letrozole/来曲唑实验方案

Letrozole/来曲唑技术信息

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Letrozole/来曲唑 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Letrozole/来曲唑 质控信息

Letrozole/来曲唑 生物活性

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Letrozole/来曲唑 动物研究

Letrozole/来曲唑 参考文献

Letrozole/来曲唑 实验方案

Letrozole/来曲唑 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

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Letrozole/来曲唑纯度/质量文件产品仅供科研

Letrozole/来曲唑质控信息

Letrozole/来曲唑生物活性

Letrozole/来曲唑细胞研究

Letrozole/来曲唑动物研究

Letrozole/来曲唑参考文献

Letrozole/来曲唑实验方案

Letrozole/来曲唑技术信息