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Letrozole
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Letrozole图片
CAS NO:112809-51-5
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
100mg电议

产品介绍
Letrozole (CGS 20267) 是一种有效的、选择性的、可逆的和口服活性的芳香酶非甾体抑制剂,IC50 为 11.5 nM。来曲唑选择性抑制雌激素的生物合成,可用于乳腺癌的研究。
Cas No.112809-51-5
别名来曲唑; CGS 20267
化学名4-[(4-cyanophenyl)-(1,2,4-triazol-1-yl)methyl]benzonitrile
Canonical SMILESC1=CC(=CC=C1C#N)C(C2=CC=C(C=C2)C#N)N3C=NC=N3
分子式C17H11N5
分子量285.3
溶解度≥ 14.265mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Letrozole is a novel and potent type (II) aromatase inhibitor with IC50 of 11.5 nM. It belongs to the reversible non-steroidal compound family which can inhibit Arom. However, there is no evidence that it can affect the adrenal steroidogenesis.[1]

Normally, Type II inhibitors have a common feature of heterocyclic azole moiety, which can be binded to the heme–iron in aromatase. It contains a structure of 1,2,4-triazole moieties which can coordinate the heme–iron of cytochrome P450. Meanwhile, benzonitrile substituted letrozole can mimic a unique enzyme structure of the substrate androstenedione.[2]

Letrozole administration can reduce spine synapse and axon outgrowth and it also will decrease the expression of estrogen receptor ? (ER?). While, the synaptic proteins including GAP-43 can impaire the long-termpotentiation.[1] Letrozole is proved to promote FSH release from the hypothalamic pituitary axis by responding to decreased estrogen (E) feedback.[3]

References:
[1] Chen Bian, Yangang Zhao, Qiang Guo, Ying Xiong, Wenqin Cai, Jiqiang Zhang. Aromatase inhibitor letrozole downregulates steroid receptor coactivator-1 in specific brain regions that primarily related to memory, neuroendocrine and integration. The Journal of Steroid Biochemistry and Molecular Biology. May 2014. 141: 37-43.
[2] Hakki Türker Akcay, Riza Bayrak. Computational studies on the anastrozole and letrozole, effective chemotherapy drugs against breast cancer. Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy. 25 March 2014. 122: 142-152.
[3] Lindsay Malloch, Alice Rhoton-Vlasak. An assessment of current clinical attitudes toward letrozole use in reproductive endocrinology practices. Fertility and Sterility. December 2013. 100(6): 1740-1744.