| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Vorozole targets aromatase (CYP19A1), the enzyme responsible for the conversion of androgens to estrogens. Vorozole is a potent and selective non-steroidal aromatase inhibitor with IC50 values of 1.9 nM (human placental) and 1.2 nM (rat ovarian). By inhibiting aromatase, Vorozole reduces estrogen biosynthesis, which is a key therapeutic strategy for hormone-dependent breast cancer.
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| ln Vitro |
In rat granulosa cells stimulated with FSH, vorozole inhibits aromatase activity with an IC50 of 1.4 nM [4].
In vitro, Vorozole is a potent aromatase inhibitor with IC50 values of 1.9 nM (human placental) and 1.2 nM (rat ovarian). The compound selectively inhibits aromatase activity in cell-free and cell-based systems. Detailed in vitro activity data, including effects on estrogen-dependent cell proliferation, have been characterized in various breast cancer cell lines. |
| ln Vivo |
In addition to having anti-tumor effects, vorozole (0.8–1.25 mg/kg; gavage; once daily for 77 days) raises serum testosterone levels and insulin-like growth factor (IGF)-1 release [3]. In ovariectomized nude mice, vorozole (oral; 5 days) completely inhibits tumor aromatase and reduces uterine weight in a dose-dependent manner [4].
In vivo, Vorozole has been studied for its effects on estrogen-dependent tumor growth in animal models of breast cancer. The compound reduces estrogen levels and inhibits the growth of hormone-dependent tumors. Detailed in vivo data regarding dosage, administration routes, and specific efficacy endpoints are limited in the available literature. |
| Enzyme Assay |
Vorozole's aromatase inhibition activity has been characterized using human placental and rat ovarian microsomal preparations. Enzyme assays typically involve measuring the conversion of androstenedione to estrone using radiolabeled substrates. Vorozole has IC50 values of 1.9 nM (human placental) and 1.2 nM (rat ovarian). Binding affinity and inhibition kinetics are determined using standard enzyme kinetic assays.
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| Cell Assay |
In vitro cell experiments with Vorozole typically use estrogen-dependent breast cancer cell lines such as MCF-7. Cells are treated with the compound at various concentrations, and cell proliferation, aromatase activity, and estrogen levels are assessed. The compound's effects on estrogen signaling and cell growth are evaluated.
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| Animal Protocol |
Animal/Disease Models: Female SD (SD (Sprague-Dawley)) rat [3]
Doses: 0.08, 0.16, 0.31, 0.63 or 1.25 mg/kg Route of Administration: gavage; daily (starting at 43 days of age) for 77 days; single dose after 7 days Results of intravenous (iv) (iv)injection of methylnitrosourea (MNU) (50 mg/kg body weight): resulted in a dose-dependent increase in weight gain, diminished cancer incidence, increased insulin-like growth factor (IGF) - 1. Serum testosterone levels. In vivo animal studies with Vorozole have been conducted using rodent models of hormone-dependent breast cancer. The compound is typically administered via oral gavage. Detailed protocols regarding dosage, treatment duration, and specific animal models are not extensively reported in the available literature. |
| ADME/Pharmacokinetics |
Pharmacokinetic data specific to Vorozole are limited in the available literature. As a small molecule, the compound is expected to have reasonable oral bioavailability and tissue penetration. Further pharmacokinetic studies are needed to fully characterize its absorption, distribution, metabolism, and excretion properties.
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| Toxicity/Toxicokinetics |
Vorozole is considered safe for research use at typical concentrations. As a research compound, it is intended for laboratory use only and not for human consumption. The compound should be handled under standard laboratory safety practices with appropriate precautions.
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| References |
[1]. Wouters W, et al. Pharmacology of vorozole. J Steroid Biochem Mol Biol. 1993 Mar;44(4-6):617-21.
[2]. Wiseman LR, et al. Vorozole. Drugs Aging. 1997 Sep;11(3):245-50; discussion 251-2. [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. |
| Additional Infomation |
Vorozole belongs to the benzotriazole class of compounds.
Vorozole (R83842) is a potent and selective non-steroidal aromatase inhibitor with IC50 values of 1.9 nM (human placental) and 1.2 nM (rat ovarian). It is used for the research of hormone-dependent breast cancer. The compound is a triazole derivative that inhibits estrogen biosynthesis by blocking the aromatase enzyme. Purity is typically ≥98%. |
| Molecular Formula |
C16H13N6CL
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|---|---|
| Molecular Weight |
324.76762
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| Exact Mass |
324.089
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| CAS # |
129731-10-8
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| PubChem CID |
6918191
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.44g/cm3
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| Boiling Point |
575.1ºC at 760 mmHg
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| Flash Point |
301.6ºC
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| Vapour Pressure |
3.15E-13mmHg at 25°C
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| Index of Refraction |
1.738
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| LogP |
2.85
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
402
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| Defined Atom Stereocenter Count |
1
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| SMILES |
ClC1C=CC(=CC=1)[C@@H](C1C=CC2=C(C=1)N(C)N=N2)N1C=NC=N1
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| InChi Key |
XLMPPFTZALNBFS-INIZCTEOSA-N
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| InChi Code |
InChI=1S/C16H13ClN6/c1-22-15-8-12(4-7-14(15)20-21-22)16(23-10-18-9-19-23)11-2-5-13(17)6-3-11/h2-10,16H,1H3/t16-/m0/s1
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| Chemical Name |
6-[(S)-(4-chlorophenyl)-(1,2,4-triazol-1-yl)methyl]-1-methylbenzotriazole
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0791 mL | 15.3955 mL | 30.7910 mL | |
| 5 mM | 0.6158 mL | 3.0791 mL | 6.1582 mL | |
| 10 mM | 0.3079 mL | 1.5396 mL | 3.0791 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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