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    Aminoglutethimide (BA-16038)
    Aminoglutethimide (BA-16038)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1802
    CAS #: 125-84-8Purity ≥98%

    Description: Aminoglutethimide (also known as BA-16038, NSC-330915) is an an anticancer drug that acts as a nonsteroidal aromatase inhibitor with IC50 of 10 μM. Aminoglutethimide decreases the production of sex hormones such as estrogen in women or testosterone in men, and suppresses the growth of tumors that need sex hormones to grow. Aminoglutethimide blocks the production of steroids derived from cholesterol and is clinically used in the treatment of Cushing's syndrome and metastatic breast cancer. 

    References: Eur J Med Chem. 2009 Oct;44(10):4121-7; Cancer Res. 1982 Aug;42(8 Suppl):3353s-3359s.

    Related CAS#: 23734-88-5 (Aminoglutethimide phosphate); 55511-44-9 [(D)-Aminoglutethimide]; 57288-03-6 [(S)-Aminoglutethimide]; 57344-88-4 [(R)-Aminoglutethimide tartrate]; 62268-19-3 [(S)-Aminoglutethimide tartrate]

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    Molecular Weight (MW)232.28
    FormulaC13H16N2O2 
    CAS No.125-84-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 20 mg/mL (86.1 mM)
    Water: <1 mg/mL
    Ethanol: 7 mg/mL (30.1 mM)
    Solubility (In vivo)1% DMSO+30% polyethylene glycol+1% Tween 80: 8 mg/mL  
    SynonymsBA-16038; NSC-330915; BA16038; NSC330915; BA 16038; NSC 330915; Ainoglutethimide; Cytadren; Orimeten; Elipten; Aminoglutetimida; Aminoglutethimidum; Ba16038; Cytadren; Prestwick243; CCRIS 7562; CHEBI:2654; Aminoglutethimidum


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    In Vitro

    In vitro activity: 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.


    Kinase Assay: 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).  


    Cell Assay: The NCI-h295 tumor cell line is maintained in RPMI 1640 medium supplemented with transferrin (0.1 mg/mL), insulin (5 μg/mL), selenium (5.2 μg/mL) and 2% FCS. The cells are incubated for 48 hours with Aminoglutethimide (3, 30, 300 μM). Then cells are examined by trypan blue staining for cell viability, counted with a coulter counter. For the assessment of ACTH-R mRNA, cells are harvested, and total RNA is extracted, electrophoresed, blotted and hybridized with a human ACTH-R cDNA probe.

    In VivoAminoglutethimide 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. 
    Animal modelSwiss CD1 male and female mice 
    Formulation & DosageDissolved in DMSO and diluted in saline; 150 mg/kg; i.p. injection 
    References

     Eur J Med Chem. 2009 Oct;44(10):4121-7; Cancer Res. 1982 Aug;42(8 Suppl):3353s-3359s.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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