Fadrozole hydrochloride hemihydrate  (Synonyms: CGS 16949A hemihydrate; (Rac)-FAD286 hydrochloride hemihydrate)

Fadrozole hydrochloride hemihydrate is an orally active, potent, selective and nonsteroidal aromatase inhibitor, with an IC₅₀ of 6.4 nM. Fadrozole hydrochloride hemihydrate inhibits the production of estrogen and progesterone, with IC₅₀ values of 0.03 and 120 μM. Fadrozole hydrochloride hemihydrate shows prevention of spontaneous tumours. Fadrozole hydrochloride hemihydrate can be used for the research of estrogen-dependent disease and cancer^[1][2][3].

Synthesis of other cytochrome P-450 dependent steroids can be suppressed to various degrees with higher doses of Fadrozole hydrochloride hemihydrate^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Fadrozole hydrochloride hemihydrate is able to inhibit the aromatase-mediated uterine hypertrophy in immature female rats with an ED₅₀ of 0.03 mg/kg when given orally^[1].
Fadrozole hydrochloride hemihydrate prevents the development of both benign and malignant spontaneus mammary neoplasns in female Sprague-Dawley rats. It also slows the spontaneous development of ptuitary pars distalis adenomas in female rats, and reduces the incidence of spontaneous hepatocellular tumours in male and female rats^[2].
Administration of Fadrozole hydrochloride hemihydrate in male and female mice accompanies with a 70% reduction in parasite burden. This protective effect is associated in male mice with a recovery of the specific cellular immune response^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

268.74

C₁₄H₁₃N₃.ClH.1/2H₂O

176702-70-8

N#CC1=CC=C(C=C1)C2CCCC3=CN=CN23.[H]Cl.[H]O[H].[1/2]

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]