Atamestane  (Synonyms: SH 489)

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)^[1].

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^[2].

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

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^[1].
Atamestane (1 and 3 mg/animal/day; subcutaneously for 3 days) inhibits ovarian estrogen biosynthesis in pregnant mare serum gonadotropin (PMSG)-primed rats^[1].
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^[2].

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

298.42

C₂₀H₂₆O₂

96301-34-7

C[C@]1([C@](CC2)([H])[C@]3([H])CCC4=CC(C=C(C)[C@]4(C)[C@@]3([H])CC1)=O)C2=O

Room temperature in continental US; may vary elsewhere.

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• [1]. M F el Etreby. Atamestane: an aromatase inhibitor for the treatment of benign prostatic hyperplasia. A short review. J Steroid Biochem Mol Biol. 1993 Mar;44(4-6):565-72.  [Content Brief]

  [2]. Gauri J Sabnis, et al. Toremifene-atamestane; alone or in combination: predictions from the preclinical intratumoral aromatase model. J Steroid Biochem Mol Biol. 2008 Jan;108(1-2):1-7.  [Content Brief]