L6545
Letrozole
≥98% (HPLC), powder, non-steroidal aromatase inhibitor
Synonym(s):
4,4′-(1H-1,2,4-Triazol-1-ylmethylene)bisbenzonitrile
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About This Item
Empirical Formula (Hill Notation):
C17H11N5
CAS Number:
Molecular Weight:
285.30
MDL number:
UNSPSC Code:
51111800
PubChem Substance ID:
NACRES:
NA.77
Product Name
Letrozole, ≥98% (HPLC)
Quality Level
Assay
≥98% (HPLC)
form
powder
color
white to off-white
solubility
DMSO: >50 mg/mL
originator
Novartis
storage temp.
2-8°C
SMILES string
N#CC(C=C1)=CC=C1C(N2C=NC=N2)C3=CC=C(C#N)C=C3
InChI
1S/C17H11N5/c18-9-13-1-5-15(6-2-13)17(22-12-20-11-21-22)16-7-3-14(10-19)4-8-16/h1-8,11-12,17H
InChI key
HPJKCIUCZWXJDR-UHFFFAOYSA-N
Gene Information
human ... CYP19A1(1588)
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Application
Letrozole has been used:
- in organoid growth assay to determine its inhibitory capacity(48)
- to investigate steroid receptor coactivator-1 (SRC-1) mediated endogenous estrogen regulation of hippocampal PSD-95(49)
- to determine its effects on tumor-induced hyperalgesia(50)
- for hormonal manipulation in rats(51)
- to study its effects on lipocalin-2 (Lcn2)(52)
- to determine its effects on mechanical hyperalgesia and aromatase expression(53)
Biochem/physiol Actions
Letrozole acts as an adjuvant agent and is used to treat breast cancer.
Letrozole is a non-steroidal aromatase inhibitor.
Letrozole is a third generation nonsteroidal aromatase inhibitor. It is a competitive inhibitor of the aromatase enzyme system and thus inhibits the conversion of androgens to estrogens. Letrozole inhibits the aromatase enzyme by competitively binding to the heme of the cytochrome P450 subunit of the enzyme, resulting in a reduction of estrogen biosynthesis in all tissues.
Features and Benefits
This compound is featured on the Nuclear Receptors (Steroids) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by Novartis. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
Signal Word
Warning
Hazard Statements
Precautionary Statements
Hazard Classifications
Repr. 2 - STOT RE 2
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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Natalia Lagunas et al.
Frontiers in neuroanatomy, 16, 902218-902218 (2022-07-12)
Sex steroid hormones, such as androgens and estrogens, are known to exert organizational action at perinatal periods and activational effects during adulthood on the brain and peripheral tissues. These organizational effects are essential for the establishment of biological axes responsible
Bianca Posocco et al.
PloS one, 15(2), e0228822-e0228822 (2020-02-08)
A novel LC-MS/MS method was developed for the quantification of the new cyclin dependent kinase inhibitors (CDKIs) palbociclib and ribociclib and the aromatase inhibitor letrozole used in combinatory regimen. The proposed method is appropriate to be applied in clinical practice
Drugs for Pregnant and Lactating Women E-Book (2009)
G Allevi et al.
British journal of cancer, 108(8), 1587-1592 (2013-04-13)
The objective of this study was to determine the optimal scheduling of 2.5 mg daily letrozole in neoadjuvant breast cancer patients to obtain pathological complete response (pathCR) and assess Ki-67 expression as an early predictor of response. This single institution
Mothaffar F Rimawi et al.
Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 31(14), 1726-1731 (2013-04-10)
We previously reported the eradication of human epidermal growth factor receptor 2 (HER2)- amplified human xenografts in mice by inhibition of the HER2 pathway with lapatinib and trastuzumab to block all homo- and heterodimer signaling as well as by blockade
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