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Kluczowe dokumenty
F3806
Fadrozole hydrochloride
≥98% (HPLC)
Synonim(y):
4-(5,6,7,8-Tetrahydroimidazo[1,5-a]pyridin-5-yl)-benzonitrile, Afema, CGS 16949A
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About This Item
Wzór empiryczny (zapis Hilla):
C14H13N3·HCl
Numer CAS:
Masa cząsteczkowa:
259.73
Numer MDL:
Kod UNSPSC:
51111800
Identyfikator substancji w PubChem:
NACRES:
NA.77
Polecane produkty
Poziom jakości
Próba
≥98% (HPLC)
Formularz
powder
rozpuszczalność
DMSO: >20 mg/mL
inicjator
Novartis
temp. przechowywania
room temp
ciąg 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
Klucz InChI
UKCVAQGKEOJTSR-UHFFFAOYSA-N
Działania biochem./fizjol.
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.
Cechy i korzyści
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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Hasło ostrzegawcze
Danger
Zwroty wskazujące rodzaj zagrożenia
Zwroty wskazujące środki ostrożności
Klasyfikacja zagrożeń
Acute Tox. 3 Oral - Repr. 2
Kod klasy składowania
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
Klasa zagrożenia wodnego (WGK)
WGK 2
Temperatura zapłonu (°F)
Not applicable
Temperatura zapłonu (°C)
Not applicable
Środki ochrony indywidualnej
dust mask type N95 (US), Eyeshields, Faceshields, Gloves
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