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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Drugs for Pregnant and Lactating Women E-Book (2009)
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
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
Lauren D Otto et al.
Frontiers in oncology, 12, 798704-798704 (2022-04-12)
Breast cancer is one of the most common diseases in the United States with 1 in 8 women developing the disease in her lifetime. Women who develop breast cancer are often post-menopausal and undergo a complex sequence of treatments including surgery, chemotherapy, and aromatase inhibitor therapy. Both independently and
Dennis C Sgroi et al.
Journal of the National Cancer Institute, 105(14), 1036-1042 (2013-07-03)
Biomarkers to optimize extended adjuvant endocrine therapy for women with estrogen receptor (ER)-positive breast cancer are limited. The HOXB13/IL17BR (H/I) biomarker predicts recurrence risk in ER-positive, lymph node-negative breast cancer patients. H/I was evaluated in MA.17 trial for prognostic performance
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