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Merck
CN

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
UNSPSC Code:
51111800
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
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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)

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.


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pictograms

Health hazard

signalword

Warning

Hazard Classifications

Repr. 2 - STOT RE 2

Storage Class

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)
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
Pamela J Goodwin et al.
Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 32(21), 2231-2239 (2014-06-18)
Obesity is associated with poor outcomes in women with operable breast cancer. Lifestyle interventions (LIs) that help women reduce their weight may improve outcomes. We conducted a multicenter randomized trial comparing mail-based delivery of general health information alone or combined



Global Trade Item Number

SKUGTIN
L6545-10MG04061833958919
L6545-50MG04061833958926