F3806

Fadrozole hydrochloride

≥98% (HPLC)

• 동의어(들): 4-(5,6,7,8-Tetrahydroimidazo[1,5-a]pyridin-5-yl)-benzonitrile, Afema, CGS 16949A
• 실험식(Hill 표기법): C₁₄H₁₃N₃·HCl
• CAS Number: 102676-31-3
• Molecular Weight: 259.73
• MDL number: MFCD00866239
• UNSPSC 코드: 51111800
• PubChem Substance ID: 329799706
• NACRES: NA.77

속성

• Quality Level: 100
• 분석: ≥98% (HPLC)
• 양식: powder
• solubility: DMSO: >20 mg/mL
• 주관자: Novartis
• 저장 온도: 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

설명

생화학적/생리학적 작용

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.

특징 및 장점

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

안전성 정보

• 픽토그램: GHS06,GHS08
• 신호어: Danger
• 유해 및 위험 성명서: H301,H361
• 예방조치 성명서: P202 - P264 - P280 - P301 + P310 - P405 - P501
• Hazard Classifications: Acute Tox. 3 Oral - Repr. 2
• Storage Class Code: 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
• 개인 보호 장비: dust mask type N95 (US), Eyeshields, Faceshields, Gloves