| CAS NO: | 176702-70-8 |
| 规格: | ≥98% |
Description:
Fadrozole HCl hydrate (CGS 16949A) is a highly potent and selective nonsteroidal
aromatase inhibitor (IC50 of 6.4 nM) with potential antineoplastic
activity. Aromatase, a member of the cytochrome P-450 superfamily, is
found in many tissues; overexpression has been linked to the development
of preneoplastic and neoplastic changes in breast tissue. Check for
active clinical trials or closed clinical trials using this agent.
Fadrozole specifically inhibits aromatase, blocking the aromatization of
androstenedione and testosterone into estrone and estradiol,
respectively, the final step in estrogen biosynthesis; the reduction in
estrogen levels may inhibit growth in estrogen-dependent cancers. References: [1]. Browne
LJ, et al. Fadrozole hydrochloride: a potent, selective, nonsteroidal
inhibitor of aromatase for the treatment of estrogen-dependent disease. J
Med Chem. 1991 Feb;34(2):725-36. [2]. Gunson
DE, et al. Prevention of spontaneous tumours in female rats by
fadrozole hydrochloride, an aromatase inhibitor. Br J Cancer. 1995
Jul;72(1):72-5. [3]. Morales-Montor
J, et al. Inhibition of p-450 aromatase prevents feminisation and
induces protection during cysticercosis. Int J Parasitol. 2002
Oct;32(11):1379-87. [4].
Brixius-Anderko S, Scott EE. Structure of human cortisol-producing
cytochrome P450 11B1 bound to the breast cancer drug fadrozole provides
insights for drug design. J Biol Chem. 2018 Nov 13. pii:
jbc.RA118.006214. doi: 10.1074/jbc.RA118.006214. Related CAS #:102676-31-3 (HCl) 176702-70-8 (HCl hydrate) 102676-47-1 (free base)
纯度：≥98%
CAS：176702-70-8
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