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Purity: ≥98%
Anastrozole (formerly known as ZD-1033) is a potent, third-generation nonsteroidal and selective inhibitor of aromatase with an IC50 of 15 nM for inhibiting human placental aromatase. Anastrozole selectively binds to and reversibly inhibits aromatase, a cytochrome P-450 enzyme complex found in many tissues including those of the premenopausal ovary, liver, and breast. Anastrozole has been reported to inhibit human placental aromatase with an IC50 value of 14.6 nM or 0.0043μg/ml.
| ln Vitro |
With an IC50 of 15 nM, anastrozozole, a very simple achiral benzyltriazole derivative, inhibits human placental aromatase. It has 200 times the potency of aminoglutethimide (AG), twice the potency of 4-OHA, and one-third the potency of fadrozole in the same assay [1].
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| ln Vivo |
On day four, groups of immature (22-day-old) female rats received subcutaneous injections of androstenedione (AD) in peanut oil (30 mg/kg) for three days. On day four, the rats either received an oral injection of different doses of anastrozozole or no injection at all. After being dissected, the uterus was dried off and weighed. On days two or three of the cycle, an oral dose of 0.1 mg/kg of anastrozozole completely prevents ovulation. In immature rats, anastrozozole totally eliminated the uterotropic action of exogenous AD at the same daily dose (0.1 mg/kg). Oral doses of anastrozozole (0.1 mg/kg and above) administered twice daily in male pig-tailed monkeys decreased circulating estradiol concentrations by 50–60% [1].
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| References |
[1]. Dukes M, et al. The preclinical pharmacology of "Arimidex" (anastrozole; ZD1033)--a potent, selective aromatase inhibitor. J Steroid Biochem Mol Biol. 1996 Jul;58(4):439-45
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| Molecular Formula |
C17H19N5
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|---|---|
| Molecular Weight |
293.37
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| CAS # |
120511-73-1
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| Related CAS # |
Anastrozole-d12;120512-32-5
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| SMILES |
CC(C1=CC(CN2N=CN=C2)=CC(C(C)(C)C#N)=C1)(C)C#N
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| Chemical Name |
2,2'-(5-((1H-1,2,4-triazol-1-yl)methyl)-1,3-phenylene)bis(2-methylpropanenitrile)
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| Synonyms |
ZD-1033; ZD1033; ZD 1033; CCRIS 9352; HSDB 7462; ICI D1033; Anastrozole (ANAS); Trade name: Arimidex.
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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) |
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| Preparing Stock Solutions | 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 |
*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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