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Fadrozole hydrochloride

Cat. No. M7802

All AbMole products are for research use only, cannot be used for human consumption.

Fadrozole hydrochloride Structure
Synonym:

CGS 16949A

Size Price Availability Quantity
5mg USD 65  USD65 In stock
10mg USD 85  USD85 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 259.73
Formula C14H13N3·HCl
CAS Number 102676-31-3
Solubility (25°C) DMSO: ≥20 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Rajeev Kharb, et al. Aromatase inhibitors: Role in postmenopausal breast cancer

[2] Monica Minnaard-Huiban, et al. Fadrozole reverses cardiac fibrosis in spontaneously hypertensive heart failure rats: discordant enantioselectivity versus reduction of plasma aldosterone

[3] A A Miller, et al. Fadrozole hydrochloride in postmenopausal patients with metastatic breast carcinoma

[4] M Dowsett, et al. Endocrine changes with the aromatase inhibitor fadrozole hydrochloride in breast cancer

[5] L J Browne, et al. Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease

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  Catalog
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Keywords: Fadrozole hydrochloride, CGS 16949A supplier, inhibitors, activators

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