F3806

Fadrozole hydrochloride

≥98% (HPLC), nonsteroidal aromatase inhibitor, powder

• Synonym(s): 4-(5,6,7,8-Tetrahydroimidazo[1,5-a]pyridin-5-yl)-benzonitrile, Afema, CGS 16949A
• Empirical Formula (Hill Notation): C₁₄H₁₃N₃·HCl
• CAS Number: 102676-31-3
• Molecular Weight: 259.73
• UNSPSC Code: 51111800
• PubChem Substance ID: 329799706
• NACRES: NA.77
• MDL number: MFCD00866239
• Assay: ≥98% (HPLC)
• Form: powder

Properties

• Product Name: Fadrozole hydrochloride, ≥98% (HPLC)
• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• solubility: DMSO: >20 mg/mL
• originator: Novartis
• storage temp.: room temp
• SMILES string: 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
• InChI key: UKCVAQGKEOJTSR-UHFFFAOYSA-N

Description

Biochem/physiol Actions

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.

Features and Benefits

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: GHS06,GHS08
• signalword: Danger
• hcodes: H301,H361
• pcodes: P202 - P264 - P280 - P301 + P310 - P405 - P501
• Hazard Classifications: Acute Tox. 3 Oral - Repr. 2
• Storage Class: 6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• wgk: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable
• ppe: dust mask type N95 (US), Eyeshields, Faceshields, Gloves