Anastrozole
Based on 4 publication(s) in Google Scholar
Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC50 of 15 nM.
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- Pureté: 99.95%
- CAS No.: 120511-73-1
- Formule: C17H19N5
- Masse moléculaire:293.37
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) Anastrozole
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Activité biologique
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Aromatase |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| JEG-3 | IC50 |
1.5 nM
Compound: anastrozole
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Inhibition of aromatase in human JEG3 cells by scintillation spectrometry
Inhibition of aromatase in human JEG3 cells by scintillation spectrometry
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[PMID: 20148564] |
| MCF7 | IC50 |
3.6 nM
Compound: Arimidex
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Inhibition of aromatase (unknown origin) transfected in human MCF7 cells
Inhibition of aromatase (unknown origin) transfected in human MCF7 cells
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[PMID: 26689671] |
Anastrozole is a comparatively simple, achiral benzyltriazole derivative, that inhibits human placental aromatase with an IC50 of 15 nM. In the same assay it is 200 times as potent as aminoglutethimide (AG), twice as potent as 4-OHA and one third as potent as Fadrozole[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 120511-73-1
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Appearance Solid
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Masse moléculaire 293.37
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Formule C17H19N5
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Color White to off-white
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SMILES
CC(C)(C#N)C1=CC(C(C)(C#N)C)=CC(CN2C=NC=N2)=C1
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Synonyms
ZD1033
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Toxicol Appl Pharmacol
In silico and in vitro assessment of drugs potentially causing adverse effects by inhibiting CYP17A1. [Abstract]2024 May:486:116945. PMID: 38688424 -
J Pharm Biomed Anal
A hydrophobic deep eutectic solvent-based vortex-assisted liquid-liquid microextraction applied for doping control of aromatase inhibitors from equine urine. [Abstract]2023 Sep 20:234:115583. PMID: 37494867 -
Drug Test Anal
High-throughput liquid chromatography tandem mass spectrometry assay as initial testing procedure for analysis of total urinary fraction. [Abstract]2021 Feb;13(2):283-298. PMID: 32852861
Solvant et solubilité
DMSO : ≥ 100 mg/mL (340.87 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.52 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.52 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
Aromatase inhibition is measured using human placental microsomes and the method of Thompson and Siiteri with Testosterone (0.5 μM) as substrate. 11-hydroxylase inhibition is determined by measuring the conversion of [1,2,6,7-3H]-ll-deoxy- cortisol to cortisol using freshly prepared mitochondria from guinea pig, dog and cow adrenal glands. Reaction products are extracted into chloroform and separated by thin layer chromatography[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Groups of at least eight adult female rats, housed in controlled lighting (on 06.00-20.00 h) and temperature (24±2°C) and undergoing 4-day oestrous cycles, are treated p.o. with a single dose of Anastrozole (0.01-0.1 mg/kg), Fadrozole (0.01-0.1 mg/kg) or AG (5-20 mg/kg) on day 2 at 16.00 h or day 3 at 12.00 h. The presence or absence of eggs in the oviducts on day 1 of the next cycle is then determined. Ovulation is considered blocked when no eggs are found.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (279 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.4087 mL | 17.0433 mL | 34.0866 mL | 85.2166 mL |
| 5 mM | 0.6817 mL | 3.4087 mL | 6.8173 mL | 17.0433 mL | |
| 10 mM | 0.3409 mL | 1.7043 mL | 3.4087 mL | 8.5217 mL | |
| 15 mM | 0.2272 mL | 1.1362 mL | 2.2724 mL | 5.6811 mL | |
| 20 mM | 0.1704 mL | 0.8522 mL | 1.7043 mL | 4.2608 mL | |
| 25 mM | 0.1363 mL | 0.6817 mL | 1.3635 mL | 3.4087 mL | |
| 30 mM | 0.1136 mL | 0.5681 mL | 1.1362 mL | 2.8406 mL | |
| 40 mM | 0.0852 mL | 0.4261 mL | 0.8522 mL | 2.1304 mL | |
| 50 mM | 0.0682 mL | 0.3409 mL | 0.6817 mL | 1.7043 mL | |
| 60 mM | 0.0568 mL | 0.2841 mL | 0.5681 mL | 1.4203 mL | |
| 80 mM | 0.0426 mL | 0.2130 mL | 0.4261 mL | 1.0652 mL | |
| 100 mM | 0.0341 mL | 0.1704 mL | 0.3409 mL | 0.8522 mL |
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