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编 号：F541016
分子式：C20H26O2
分子量：298.42
分子式：C20H26O2
分子量：298.42
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CAS No: 96301-34-7
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生物活性：
Atamestane (SH 489) is a specific aromatase inhibitor, which selectively blocks the estrogen biosynthesis resulting from the aromatization of androstenedione and testosterone. Atamestane is a competitive and irreversible inhibitor of estrogen biosynthesis. Atamestane can be used for the research of benign prostatic hyperplasia (BPH).
体内研究：
Atamestane is a selective, pure, and highly effective steroidal aromatase inhibitor, with an excellent safety profile. Atamestane completely antagonizes all the estrogen-induced changes in the prostate. Atamestane leads to a decrease of pregnant mare serum gonadotropin-stimulated ovarian estrogen production, and inhibits androstenedione-induced estrogenic effects such as uterine growth and abortion in rats. Atamestane inhibits estrogen-related negative feedback. Atamestane is highly effective in inhibiting estrogen-induced hyperplastic changes in the fibromuscular stroma of the prostate in androstenedione-treated dogs and monkeys.Atamestane (1 and 3 mg/animal/day; subcutaneously for 3 days) inhibits ovarian estrogen biosynthesis in pregnant mare serum gonadotropin (PMSG)-primed rats.The combination of Toremifene (1000μg/day) plus Atamestane (1000μg/day) is as effective as Toremifene or Tamoxifen (100μg/day) alone but may not provide any additional benefit over Toremifene alone or Tamoxifen alone in ovariectomized female SCID mice bearing Ac-1 xenografts.Animal Model:Infantile female rats, weighing about 50 g
Dosage:1 and 3 mg/animal/day
Administration:Subcutaneously for 3 days
Result:Resulted in a significant dose-dependent decrease of the pregnant mare serum gonadotropin (PMSG)-induced, elevated serum estrogen concentration.
Animal Model:Ovariectomized female SCID mice bearing Ac-1 xenografts
Dosage:Atamestane (1000 μg/day), or the combination of Toremifene (1000 μg/day) plus Atamestane (1000 μg/day)
Administration:Injected subcutaneously
Result:Caused dose dependent reductions in mean tumor weights. The doses of Toremifene and Atamestane which caused maximum reduction in tumor growth were selected for the combination study.
体外研究：
Atamestane inhibits the growth of Ac-1 cells in vitro with IC50 value of 60.4±17.2 μM. The combination of Toremifene plus Atamestane is better than Toremifene or Atamestane alone in vitro.
Atamestane (SH 489) is a specific aromatase inhibitor, which selectively blocks the estrogen biosynthesis resulting from the aromatization of androstenedione and testosterone. Atamestane is a competitive and irreversible inhibitor of estrogen biosynthesis. Atamestane can be used for the research of benign prostatic hyperplasia (BPH).
体内研究：
Atamestane is a selective, pure, and highly effective steroidal aromatase inhibitor, with an excellent safety profile. Atamestane completely antagonizes all the estrogen-induced changes in the prostate. Atamestane leads to a decrease of pregnant mare serum gonadotropin-stimulated ovarian estrogen production, and inhibits androstenedione-induced estrogenic effects such as uterine growth and abortion in rats. Atamestane inhibits estrogen-related negative feedback. Atamestane is highly effective in inhibiting estrogen-induced hyperplastic changes in the fibromuscular stroma of the prostate in androstenedione-treated dogs and monkeys.Atamestane (1 and 3 mg/animal/day; subcutaneously for 3 days) inhibits ovarian estrogen biosynthesis in pregnant mare serum gonadotropin (PMSG)-primed rats.The combination of Toremifene (1000μg/day) plus Atamestane (1000μg/day) is as effective as Toremifene or Tamoxifen (100μg/day) alone but may not provide any additional benefit over Toremifene alone or Tamoxifen alone in ovariectomized female SCID mice bearing Ac-1 xenografts.Animal Model:Infantile female rats, weighing about 50 g
Dosage:1 and 3 mg/animal/day
Administration:Subcutaneously for 3 days
Result:Resulted in a significant dose-dependent decrease of the pregnant mare serum gonadotropin (PMSG)-induced, elevated serum estrogen concentration.
Animal Model:Ovariectomized female SCID mice bearing Ac-1 xenografts
Dosage:Atamestane (1000 μg/day), or the combination of Toremifene (1000 μg/day) plus Atamestane (1000 μg/day)
Administration:Injected subcutaneously
Result:Caused dose dependent reductions in mean tumor weights. The doses of Toremifene and Atamestane which caused maximum reduction in tumor growth were selected for the combination study.
体外研究：
Atamestane inhibits the growth of Ac-1 cells in vitro with IC50 value of 60.4±17.2 μM. The combination of Toremifene plus Atamestane is better than Toremifene or Atamestane alone in vitro.
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