F3806

Fadrozole hydrochloride

≥98% (HPLC)

• Synonyme(s) : 4-(5,6,7,8-Tetrahydroimidazo[1,5-a]pyridin-5-yl)-benzonitrile, Afema, CGS 16949A
• Formule empirique (notation de Hill) : C₁₄H₁₃N₃·HCl
• CAS Number: 102676-31-3
• Poids moléculaire : 259.73
• Numéro MDL: MFCD00866239
• Code UNSPSC : 51111800
• ID de substance PubChem : 329799706
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Essai: ≥98% (HPLC)
• Forme: powder
• Solubilité: DMSO: >20 mg/mL
• Auteur: Novartis
• Température de stockage: room temp
• Chaîne SMILES: Cl.N#Cc1ccc(cc1)C2CCCc3cncn23
• InChI: 1S/C14H13N3.ClH/c15-8-11-4-6-12(7-5-11)14-3-1-2-13-9-16-10-17(13)14;/h4-7,9-10,14H,1-3H2;1H
• Clé InChI: UKCVAQGKEOJTSR-UHFFFAOYSA-N

Description

Actions biochimiques/physiologiques

Fadrozole is a nonsteroidal aromatase inhibitor.

Fadrozole is a nonsteroidal aromatase inhibitor. Fadrozole is a very potent and highly selective inhibitor of the aromatase enzyme system in vitro and estrogen biosynthesis in vivo. It inhibited the conversion of [4-14C]androstenedione to [4-14C]estrone by human placental microsomes in a competitive manner (Ki = 1.6 nM). At a substrate concentration 3-fold the Km, Fadrozole was 180 times more potent, as an inhibitor, than aminoglutethimide (Cat. No. A9657), exhibiting half-maximal inhibition at 1.7 nM as compared to 0.3 μM. In vivo, Fadrozole lowered ovarian estrogen synthesis by gonadotropin-primed, androstenedione treated, immature rats by 90% at a dose of 260 μg/kg (PO). In vivo, Fadrozole leads to sequelae of estrogen deprivation (e.g. regression of DMBA-induced mammary tumors) without causing adrenal hypertrophy in adult rats. It blocked aromatase by 50% in human breast cancer homogenates, live breast cancer cells, human placental microsomes, and porcine ovarian microsomes at concentrations of 0.008 to 0.02 μM.

Caractéristiques et avantages

This compound was developed by Novartis. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Informations sur la sécurité

• Pictogrammes: GHS06,GHS08
• Mention d'avertissement: Danger
• Mentions de danger: H301,H361
• Conseils de prudence: P202 - P264 - P280 - P301 + P310 - P405 - P501
• Classification des risques: Acute Tox. 3 Oral - Repr. 2
• Code de la classe de stockage: 6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• Classe de danger pour l'eau (WGK): WGK 2
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable
• Équipement de protection individuelle: dust mask type N95 (US), Eyeshields, Faceshields, Gloves