Fadrozole

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Fadrozole (CGS 16949A free base) 是一种有效，选择性和非甾体类的?aromatase?抑制剂，IC50?值为6.4 nM。

A potent and selective, orally bioavailable aromatase inhibitor with IC50 of 1.7 nM, 180 times more potent than aminoglutethimide; lowers ovarian estrogen synthesis by gonadotropin-primed, androstenedione treated mice, suppresses hormone-dependent and -independent tumors in vivo.Breast Cancer Approved(In Vitro):Fadrozole hydrochloride is a very potent inhibitor of both human placental and rat ovarian aromatase. In hamster ovarian slices, fadrozole hydrochloride inhibits the production of estrogen with an IC50 of 0.03 μM. The production of progesterone is inhibited with an IC50 of 120 μM. Synthesis of other cytochrome P-450 dependent steroids can be suppressed to various degrees with higher doses of fadrozole hydrochloride. . (In Vivo):Fadrozole hydrochloride is able to inhibit the aromatase-mediated androstenedione-induced uterine hypertrophy in immature female rats with an ED50 of 0.03 mg/kg when given orally. In the same model, aminoglutethimide elicits the same effect with an ED50 of 30 mg/kg when given orally. Fadrozole hydrochloride 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 dta mas in female rats, and reduces the of spontaneous hcu ar tumours in male and female rats. Administration of fadrozole in male and female mice suppresses the production of 17b-estradiol, accompanied with a 70% reduction in parasite burden. This protective effect is associated in male mice with a recovery of the specific cellular immune response. Interleukin-6 (IL-6) serum levels, and its production by splenocytes, is augmented by 80%, together with a 10-fold increase in its expression in testes of infected male mice. Fadrozole treatment returns these levels to baseline values.

Fadrozole hydrochloride is a very potent inhibitor of both human placental and rat ovarian aromatase. In hamster ovarian slices, fadrozole hydrochloride inhibits the production of estrogen with an IC50 of 0.03 μM. The production of progesterone is inhibited with an IC50 of 120 μM. Synthesis of other cytochrome P-450 dependent steroids can be suppressed to various degrees with higher doses of fadrozole hydrochloride.

Fadrozole hydrochloride is able to inhibit the aromatase-mediated androstenedione-induced uterine hypertrophy in immature female rats with an ED50 of 0.03 mg/kg when given orally. In the same model, aminoglutethimide elicits the same effect with an ED50 of 30 mg/kg when given orally. Fadrozole hydrochloride 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 dta mas in female rats, and reduces the of spontaneous hcu ar tumours in male and female rats. Administration of fadrozole in male and female mice suppresses the production of 17b-estradiol, accompanied with a 70% reduction in parasite burden. This protective effect is associated in male mice with a recovery of the specific cellular immune response. Interleukin-6 (IL-6) serum levels, and its production by splenocytes, is augmented by 80%, together with a 10-fold increase in its expression in testes of infected male mice. Fadrozole treatment returns these levels to baseline values.

CGS 16949A | FAD286 | FAD 286

Metabolic Enzyme/Protease

CYPs

CYPs

Cancer

Breast Cancer

102676-47-1

223.279

C14H13N3

>98% (HPLC)

DMSO : ≥ 100 mg/mL 447.89 mM

C1CC(N2C=NC=C2C1)C3=CC=C(C=C3)C#N

4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)benzonitrile

(-20℃)

With Ice Pack

≥ 2 years