Anastrozole (ZD-1033)

Catalog No.S1188

For research use only.

Anastrozole (ZD-1033) is a third-generation nonsteroidal selective aromatase inhibitor. It may offer greater selectivity compared with other aromatase inhibitors, being without any intrinsic endocrine effects and with no apparent effect on the synthesis of adrenal steroids.

Anastrozole (ZD-1033) Chemical Structure

CAS No. 120511-73-1

Selleck's Anastrozole (ZD-1033) has been cited by 16 publications

Purity & Quality Control

Choose Selective Aromatase Inhibitors

Other Aromatase Products

Biological Activity

Description Anastrozole (ZD-1033) is a third-generation nonsteroidal selective aromatase inhibitor. It may offer greater selectivity compared with other aromatase inhibitors, being without any intrinsic endocrine effects and with no apparent effect on the synthesis of adrenal steroids.
Targets
Aromatase [1]
(human placental microsomes)
15 nM
In vitro

Anastrozole has high intrinsic potency in vitro and inhibits human placental aromatase with an IC50 of 15 nM. Anastrozole it is 200 times as potent as AG, twice as potent as 4-OHA and one third as potent as fadrozole. [1]. Anastrozole inhibits aromatase by binding competitively to the hem group of the CYP unit of the enzyme thereby reducing estrogen biosynthesis in the periphery and the breast. Anastrozole has little or no effect on other steroid hormones. [2]

In vivo Anastrozole (0.1 mg/kg) given orally to mature rats on Day 2 or 3 of the estrous cycle, blocked ovulation in mature females; in pubertal rats, the same dose given for 3 days completely blocks androstenedione-stimulated uterine development. These effects may be attributes to inhibition of the normal preovulatory rise in ovarian follicular estrogen synthesis in mature females and to inhibition of metabolism of the exogenous androstenedione by the immature ovary in prepubertal females. Twice-daily administration of >9.1 mg/kg of Anastrozole given orally to male pigtailed monkeys inhibits peripheral aromatase, thereby reducing circulating estradiol concentrations by 50% to 60%. [2]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 293.37
Formula

C17H19N5

CAS No. 120511-73-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)(C#N)C1=CC(=CC(=C1)CN2C=NC=N2)C(C)(C)C#N

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg 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.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04714619 Active not recruiting Drug: CB-103 Advanced Breast Cancer MedSIR|Cellestia Biotech AG May 6 2021 Phase 2
NCT04227327 Recruiting Drug: Abemaciclib|Drug: Aromatase Inhibitors Advanced Breast Cancer University of Milano Bicocca January 7 2020 Phase 2
NCT03229499 Active not recruiting Drug: Anastrozole|Drug: Placebo Oral Tablet Pulmonary Arterial Hypertension University of Pennsylvania|National Heart Lung and Blood Institute (NHLBI)|Johns Hopkins University|University of Colorado Denver|Rhode Island Hospital|Stanford University|Vanderbilt University|Washington University School of Medicine December 7 2017 Phase 2
NCT03314298 Completed Drug: testosterone anastrozole Mammographic Density Havah Therapeutics Pty Ltd August 14 2017 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Anastrozole (ZD-1033) | Anastrozole (ZD-1033) supplier | purchase Anastrozole (ZD-1033) | Anastrozole (ZD-1033) cost | Anastrozole (ZD-1033) manufacturer | order Anastrozole (ZD-1033) | Anastrozole (ZD-1033) distributor