Home Endocrinology & Hormones Aromatase inhibitor Anastrozole For research use only.

Anastrozole

Synonyms: ZD-1033

Anastrozole 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 Chemical Structure

Anastrozole Chemical Structure

CAS No. 120511-73-1

Purity & Quality Control

Anastrozole Related Products

Signaling Pathway

Aromatase Signaling Pathways

Aromatase Signaling Pathway

Biological Activity

Description Anastrozole 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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06154590 Not yet recruiting
Metastatic Breast Cancer|Tumor|Muscle Neoplasms|Chronic Pain
DR. DIANE CHISESI NFS. MD. PHD.|IRB|Paradyne Networks A Foundation
 July 2024 --
NCT04714619 Terminated
Advanced Breast Cancer
MedSIR|Cellestia Biotech AG
 May 6 2021 Phase 2
NCT04227327 Active not recruiting
Advanced Breast Cancer
University of Milano Bicocca
 January 7 2020 Phase 2

Chemical Information & Solubility

Molecular Weight 293.37 Formula

C17H19N5
CAS No. 120511-73-1 SDF Download Anastrozole SDF
Smiles CC(C)(C#N)C1=CC(=CC(=C1)CN2C=NC=N2)C(C)(C)C#N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 59 mg/mL ( (201.11 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 59 mg/mL

Water : Insoluble


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In vivo
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In vivo Formulation Calculator

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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.

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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

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