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.
For research use only. We do not sell to patients.
- CAS No.: 129731-10-8
- Formula: C16H13ClN6
- Molecular Weight:324.77
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
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Aromatase |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| JEG-3 | IC50 |
44.2 nM
Compound: (S)-vorozole
|
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
|
[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] |
In Vitro
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. Further protocols information, click here.
In Vivo
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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Molecular Weight 324.77
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
Purity & Documentation
References
[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)