L6545

Letrozole

≥98% (HPLC), powder, non-steroidal aromatase inhibitor

• Synonym(s): 4,4′-(1H-1,2,4-Triazol-1-ylmethylene)bisbenzonitrile
• Empirical Formula (Hill Notation): C₁₇H₁₁N₅
• CAS Number: 112809-51-5
• Molecular Weight: 285.30
• MDL number: MFCD00866241
• UNSPSC Code: 51111800
• PubChem Substance ID: 329817641
• NACRES: NA.77

Properties

• product name: Letrozole, ≥98% (HPLC)
• 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)

Description

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 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.

Safety Information

• Pictograms: GHS08
• Signal Word: Warning
• Hazard Statements: H361fd,H373
• Precautionary Statements: P202 - P260 - P280 - P308 + P313 - P405 - P501
• 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