Catalog No.S1672 Synonyms: BA-16038, NSC-330915
Molecular Weight(MW): 232.28
Aminoglutethimide is an aromatase inhibitor with IC50 of 10 μM.
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Choose Selective Aromatase Inhibitors
|Description||Aminoglutethimide is an aromatase inhibitor with IC50 of 10 μM.|
|Features||A first-generation aromatase inhibitor used for estrogen-dependent breast cancer.|
Aminoglutethimide displays aromatase inhibition in vitro assay with human placental aromatase, which is an enzyme involved in the conversion of androgens into estrogens, and an important target for the endocrine treatment of breast cancer.  Aminoglutethimide inhibits ACTH receptor (ACTH-R) mRNA expression in ovine adrenocortical cells in a time-dependent fashion. Aminoglutethimide significantly suppresses steroid secretion and the baseline ACTH-R mRNA expression in a dose-dependent fashion (300 μM AG, 5±1%; 30 μM AG, 64±1%; 3 μM AG, 108±19% compared with control cells, 100±11%) by affecting the gene expression or by decreasing transcript accumulation via an effect on RNA stability, in the human NCI-h295 adrenocortical carcinoma cell line, which expresses functional ACTH receptors and produces steroids of the glucocorticoid, mineralocorticoid and androgen pathway.  Aminoglutethimide inhibits aromatase in a dose-dependent fashion with IC50 of 13 μM in 6 breast tumor homogenates, placental aromatase with IC50 of 6 μM and hypothalamic aromatase with IC50 of 8 μM. 
|In vivo||Aminoglutethimide accelerates its own metabolism from a basal value of 2.6±0.3 (S.E.) liters/24 hours to 5.3±1.4 liters/24 hours after 1 to 2 weeks of Aminoglutethimide administration, and markedly accelerates the metabolism of the synthetic glucocorticoid and dexamethasone, from basal values of 145±26.6 liters/24 hours to 568±127 liters/24 hours (p < 0.02) after 2 weeks of Aminoglutethimide administration.  Aminoglutethimide (150 mg/kg) abolishes the induction of ornithine decarboxylase (ODC) and almost depletes the gonads and plasma of progesterone or testosterone elicited by human chorionic gonadotropin (hCG) in the ovary of adult female mice and the testis of immature male mice, which is related to an inhibition of cAMP-dependent protein kinase (IC50 287 μM) rather than blockade of the steroidogenic pathway. |
|Kinase Assay: ||
Concentration–response and kinetic studies:The microsomal protein (30 μg), [1β-3H]androstenedione (6.6 × 105 dpm) and NADPH (270 μM) are used for the concentration–response experiment with an incubation time of 20 minutes. The Aminoglutethimide is initially tested at 10 μM and 100 μM concentrations, followed by a full concentration–response study with at least 8 concentrations ranging from 0.01 μM to 160 μM. For the initial velocity study the concentration of [1β-3H]androstenedione is varied from 7.5 to 100 nM and the incubation time is set to 5 minutes. The tritiated water formed during the conversion of the tritiated substrate, [1β-3H]androstenedione, to estrone is quantified by liquid scintillation counting. Each assay is performed three times in duplicate and the results are treated by nonlinear regression analysis allowing the determination of the half-maximal inhibitory concentration (IC50).
-  Neves MA, et al. Eur J Med Chem, 2009, 44(10), 4121-4127.
-  Fassnacht M, et al. J Endocrinol, 1998, 159(1), 35-42.
-  Santen RJ, et al. Cancer Res, 1982, 42(8 Suppl), 3353s-3359s.
|In vitro||DMSO||20 mg/mL (86.1 mM)|
|Ethanol||7 mg/mL (30.13 mM)|
|In vivo||Add solvents individually and in order:
1% DMSO+30% polyethylene glycol+1% Tween 80
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT00006371||Terminated||Prostate Cancer||H. Lee Moffitt Cancer Center and Research Institute|National Cancer Institute (NCI)|Janssen Pharmaceuticals||May 2000||Phase 2|
|NCT00309491||Completed||Early-stage Breast Cancer||Austrian Breast & Colorectal Cancer Study Group||December 1990||Phase 3|
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