Vorozole
Vorozole is a potent and selective, orally active non-steroidal aromatase inhibitor. Vorozole shows antitumor activity in vivo. Vorozole has the potential for the research of mammary cancer.
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- CAS No.: 129731-10-8
- Formule: C16H13ClN6
- Masse moléculaire:324.77
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
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Aromatase |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| JEG-3 | IC50 |
44.2 nM
Compound: (S)-vorozole
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Inhibition of aromatase activity in human JEG3 cells
Inhibition of aromatase activity in human JEG3 cells
|
[PMID: 18590272] |
| JEG-3 | IC50 |
29 nM
Compound: 128
|
Inhibition of aromatase (unknown origin) expressed in JEG-3 cells
Inhibition of aromatase (unknown origin) expressed in JEG-3 cells
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[PMID: 25992880] |
| JEG-3 | IC50 |
>10000 nM
Compound: 128
|
Inhibition of STS activity (unknown origin) expressed in JEG-3 cells
Inhibition of STS activity (unknown origin) expressed in JEG-3 cells
|
[PMID: 25992880] |
Vorozole inhibits aromatase activity with an IC50s of 1.4 nM in FSH-stimulated rat granulosa cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Vorozole (p.o.; 5 days) dose-dependently reduced uterus weight and completely inhibited tumor aromatase in ovariectomized nude mice[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Sprague-Dawley rats[3]
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Dosage:0.08, 0.16, 0.31, 0.63 or 1.25 mg/kg
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Administration:Gavage; daily (starting at 43 days of age) for 77 days; given a single i.v. dose of methylnitrosourea (MNU) (50 mg/kg body wt) after 7 days
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Result:Caused a dose-dependent increase in body weight gain and decrease in cancer incidence, increased the insulin-like growth factor (IGF)-1, serum testosterone levels.
Chemical Information
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CAS No. 129731-10-8
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Masse moléculaire 324.77
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Formule C16H13ClN6
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SMILES
CN1N=NC2=CC=C([C@H](C3=CC=C(Cl)C=C3)N4N=CN=C4)C=C21
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Synonyms
(+)-Vorozole; R83842
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Wouters W, et al. Pharmacology of vorozole. J Steroid Biochem Mol Biol. 1993 Mar;44(4-6):617-21. [Content Brief]
[2]. Wiseman LR, et al. Vorozole. Drugs Aging. 1997 Sep;11(3):245-50; discussion 251-2. [Content Brief]
[3]. Lubet RA,et al. Chemopreventive effects of the aromatase inhibitor vorozole (R 83842) in the methylnitrosourea-induced mammary cancer model. Carcinogenesis. 1998 Aug;19(8):1345-51. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)