For research use only.

Catalog No.S1188 Synonyms: ZD-1033

9 publications

Anastrozole Chemical Structure

Molecular Weight(MW): 293.37

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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10mM (1mL in DMSO) USD 130 In stock
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Selleck's Anastrozole has been cited by 9 publications

2 Customer Reviews

  • Cell viability analysis of BCSCs transduced as in A and treated with Anastrozole or Docetaxel, alone or in combination with BKM120 up to 72 hours. Data are mean ± SD of 3 independent experiments.

    Oncotarget, 2016, 7(34):54157-54173. Anastrozole purchased from Selleck.

    Expression of ER, PR, Bcl-2 and HER receptors in MCF-7 and AI-resistant cell lines. Western blot analysis of protein expression in AI-resistant cell lines grown under standard conditions with their respective AI and MCF-7 cells grown with 1% FCS or grown with 10% NCS + 10−7 M testosterone for 21 weeks. β-actin was used as loading control.

    Int J Oncol, 2015, 46(4):1481-90. . Anastrozole purchased from Selleck.

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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.
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]


Solubility (25°C)

In vitro DMSO 59 mg/mL (201.11 mM)
Ethanol 59 mg/mL (201.11 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 293.37


CAS No. 120511-73-1
Storage powder
in solvent
Synonyms ZD-1033
Smiles CC(C)(C#N)C1=CC(=CC(=C1)C[N]2C=NC=N2)C(C)(C)C#N

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
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
NCT02779751 Active not recruiting Drug: Abemaciclib|Drug: Pembrolizumab|Drug: Anastrozole Non Small Cell Lung Cancer|Breast Cancer Eli Lilly and Company|Merck Sharp & Dohme Corp. November 14 2016 Phase 1
NCT02095184 Recruiting Drug: Anastrozole|Drug: Letrozole Breast Cancer University of Maryland Baltimore May 25 2015 Not Applicable

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Aromatase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID