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Anastrozole Aromatase inhibitor

Cat.No.S1188

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.
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Quality Control

Batch: Purity: 99.99%
99.99

Solubility

In vitro
Batch:

DMSO : 59 mg/mL (201.11 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 59 mg/mL

Water : Insoluble

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In vivo
Batch:

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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 293.37 Formula

C17H19N5

Storage (From the date of receipt)
CAS No. 120511-73-1 Download SDF Storage of Stock Solutions

Synonyms ZD-1033 SMILES CC(C)(C#N)C1=CC(=CC(=C1)CN2C=NC=N2)C(C)(C)C#N

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Mechanism of Action

Targets/IC50/Ki
Aromatase
(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. This compound is 200 times as potent as AG, twice as potent as 4-OHA and one third as potent as fadrozole. . This chemical 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. It has little or no effect on other steroid hormones.
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 this compound given orally to male pigtailed monkeys inhibits peripheral aromatase, thereby reducing circulating estradiol concentrations by 50% to 60%.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-09-29)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07190443 RECRUITING
Breast Cancer; Locoregional Recurrence; Abemaciclib; Endocrine Therapy
Japanese Foundation for Cancer Research
2025-02-07 PHASE3
NCT05512364 RECRUITING
ER-positive Breast Cancer; HER2-negative Breast Cancer; Stage IIB Breast Cancer; Stage III Breast Cancer
European Organisation for Research and Treatment of Cancer - EORTC
2023-12-15 PHASE3
NCT06223698 NOT_YET_RECRUITING
Breast Cancer
Region Örebro County
2025-05-02 PHASE3
NCT07729046 NOT_YET_RECRUITING
Metastatic Invasive Breast Cancer; Resistant Breast Cancer; ER+, HER2-, Metastatic Breast Cancer
University of California, San Diego
2027-07 PHASE2
NCT07581834 RECRUITING
Breast Diseases; Breast Neoplasms; Dalpiciclib; Endocrine Breast Diseases; CDK4/6 Inhibitor; HR+/HER2- Breast Cancer
Fujian Cancer Hospital
2026-01-21 PHASE2
NCT07179939 NOT_YET_RECRUITING
HER2-positive Breast Cancer
Fudan University
2025-09-10 PHASE2

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