2. Metabolic Enzyme/Protease
  3. Cytochrome P450
  4. Anastrozole

Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC50 of 15 nM.

For research use only. We do not sell to patients.

Anastrozole Chemical Structure

Anastrozole Chemical Structure

CAS No. : 120511-73-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 61 In-stock
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10 mM * 1 mL in DMSO USD 61 In-stock
Solid
5 mg USD 35 In-stock
10 mg USD 55 In-stock
50 mg USD 99 In-stock
100 mg USD 154 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Anastrozole:

Anastrozole Related Antibodies

Top Publications Citing Use of Products

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC50 of 15 nM.

IC50 & Target

Aromatase

 

In Vitro

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.

Anastrozole Related Antibodies
In Vivo

Groups of eight immature (22-day-old) female rats are given androstenedione (AD) (30 mg/kg) in arachis oil s.c. daily for 3 days with or without various doses of Anastrozole p.o. on day 4 the uteri are dissected, blotted and weighed. An oral dose of 0.1 mg/kg of Anastrozole given on day 2 or day 3 of the cycle completely blocked ovulation. At the same daily dosage (0.1 mg/kg), Anastrozole completely extinguished the uterotrophic activity of exogenous AD in immature rats. In male pigtailed monkeys, twice-daily oral treatment with 0.1 mg/kg and above of Anastrozole reduced circulating oestradiol concentrations by 50-60%[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

293.37

Formula

C17H19N5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C)(C#N)C1=CC(C(C)(C#N)C)=CC(CN2C=NC=N2)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.99%

COA (253 KB) LCMS (92 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

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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Anastrozole Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Anastrozole120511-73-1ZD1033ZD 1033ZD-1033Cytochrome P450CYPsInhibitorinhibitorinhibit

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