Anastrozole (Synonyms: Anastrol, ICID 1033, ZD 1033) |
| Catalog No.GC10256 |
El anastrozol es un potente inhibidor de la aromatasa altamente selectivo que inhibe la aromatasa placentaria humana con una IC50 de 15 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 120511-73-1
Sample solution is provided at 25 µL, 10mM.
Anastrozole (Arimidex,ZD1033) is a potent and selective inhibitor of aromatase with an IC50 value of 14.6 nM or 0.0043μg/ml [1].
Anastrozole has been reported to inhibit human placental aromatase with an IC50 value of 14.6 nM or 0.0043μg/ml. In addition, an oral concentration of 0.1mg/kg of anastrozole has been revealed to completely inhibit ovulation by given on day 2 or day 3 of the cycle. In immature rat, an oral concentration of 0.1mg/kg of anastrozole has also noted to completely extinguish the uterotrophic activity of exogenous AD. Apart from these, by guinea pig, dog and cow adrenal microsomes, anastrozole has been exhibited to suppress the conversion of 11-deoxycortisol to cortisol with mean IC50 values of 4.09μM,129μM and 11.9μM, respectively [1].
References:
[1] Dukes M1, Edwards PN, Large M, Smith IK, Boyle T. The preclinical pharmacology of "Arimidex" (anastrozole; ZD1033)--a potent, selective aromatase inhibitor. J Steroid Biochem Mol Biol. 1996 Jul;58(4):439-45.
| Cell experiment [1]: | |
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Cell lines |
MCF7, HepG2, and PC3 cell lines |
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Preparation method |
The solubility of this compound in DMSO is >14.2mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
25-400 μg/mL, 24h |
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Applications |
In MCF7, HepG2, and PC3 cell lines, Anastrozole at 400 μg/mL showed the most significant cytotoxic toward all cell lines. Anastrozole at 400 μg/mL exhibited inhibition rates of 58.4%, 41.7% and 26.6% on MCF7, HepG2, and PC3 cell lines, respectively. In MCF7 breast cancer cells, Anastrozole (200 μg/mL) increased nuclear intensity corresponding to apoptotic changes by 38% and increased cell membrane permeability by 17.3%. Anastrozole also significantly increased cytochrome c release. |
| Animal experiment [2]: | |
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Animal models |
adult female rats; mature male pigtailed monkeys (M. nernestrina) |
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Dosage form |
Rats: 0.01-0.1 mg/kg, p.o., on day 2 at 16.00 h or day 3 at 12.00 hMonkeys: 0.003, 0.01, 0.03, 0.1, 0.3 and 1.0 mg/kg, p.o., twice daily (09.00 h and 16.00 h) |
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Application |
In adult female rats, Anastrozole (0.1 mg/kg) given on day 2 or day 3 completely blocked ovulation. In male pigtailed monkeys, Anastrozole (0.1 mg/kg and above) reduced circulating oestradiol concentrations by 50-60%. The clearance half-life of anastrozole in the monkey was about 7h. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Hassan F1, El-Hiti GA, Abd-Allateef M, et al. Cytotoxicity anticancer activities of anastrozole against breast, liver hepatocellular, and prostate cancer cells. Saudi Med J. 2017 Apr;38(4):359-365. [2] Dukes M1, Edwards PN, Large M, Smith IK, Boyle T. The preclinical pharmacology of "Arimidex" (anastrozole; ZD1033)--a potent, selective aromatase inhibitor. J Steroid Biochem Mol Biol. 1996 Jul;58(4):439-45. | |
| Cas No. | 120511-73-1 | SDF | |
| Sinónimos | Anastrol, ICID 1033, ZD 1033 | ||
| Chemical Name | 2-[3-(2-cyanopropan-2-yl)-5-(1,2,4-triazol-1-ylmethyl)phenyl]-2-methylpropanenitrile | ||
| Canonical SMILES | CC(C)(C#N)C1=CC(=CC(=C1)CN2C=NC=N2)C(C)(C)C#N | ||
| Formula | C17H19N5 | M.Wt | 293.37 |
| Solubility | ≥ 14.15mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4087 mL | 17.0433 mL | 34.0866 mL |
| 5 mM | 0.6817 mL | 3.4087 mL | 6.8173 mL |
| 10 mM | 0.3409 mL | 1.7043 mL | 3.4087 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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