Letrozole

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Chemical Structure| 112809-51-5 同义名 : CGS 20267
CAS号 : 112809-51-5
货号 : A278180
分子式 : C17H11N5
纯度 : 95%
分子量 : 285.3
MDL号 : MFCD00866241
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

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
动物实验配方：

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

PO 0.5% CMC-Na 50 mg/mL suspension

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].
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
实验方案
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
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.