AZD9496

Catalog No.S8372

For research use only.

AZD9496 is an oral estrogen receptor inhibitor that blocks the growth of ER-positive and ESR1 mutant breast tumours in preclinical models.

AZD9496 Chemical Structure

CAS No. 1639042-08-2

Selleck's AZD9496 has been cited by 2 Publications

1 Customer Review

Purity & Quality Control

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Biological Activity

Description AZD9496 is an oral estrogen receptor inhibitor that blocks the growth of ER-positive and ESR1 mutant breast tumours in preclinical models.
Targets
estrogen receptor [1]
In vitro

AZD9496 showed pmol/L equipotent binding to both ERα and ERβ isoforms. AZD9496 directly targets ERα for downregulation in vitro. And it also antagonizes and downregulates mutant ER in vitro and in vivo. The IC50s of ERα binding, ERα downregulation, ERα antagonism for AZD9496 are 0.82, 0.14 and 0.28 nM, respectively[1].

In vivo AZD9496 showed high oral bioavailability across three species (F% 63, 91, and 74, rat, mouse, and dog, respectively) with generally low volume and clearance across species, albeit a higher clearance in mouse. The percent free levels in human plasma of 0.15% were 5-fold higher than those measured for fulvestrant. AZD9496 is a potent, oral inhibitor of breast tumor growth in vivo. AZD9496 causes tumor regressions in combination with PI3K pathway and CDK4/6 inhibitors and in an estrogen-deprived ER+ model of resistance. This effect was accompanied by a dose-dependent decrease in PR protein levels. AZD9496 is currently being evaluated in a phase I clinical trial[1].

Protocol (from reference)

Cell Research:[1]
  • Cell lines: MCF-7 cells
  • Concentrations: 100 nM
  • Incubation Time: 0, 10, 20, 30, 40, 50 h
  • Method: Cells were grown in steroid-free conditions in SILAC media containing 13C615N4 L-arginine to label ERα peptide as "heavy" and then switched to grow in media containing unlabeled l-arginine to label newly synthesized protein as "normal" with 0.1% DMSO, 300 nmol/L tamoxifen, 100 nmol/L AZD9496, or 100 nmol/L fulvestrant for the time indicated.
Animal Research:[1]
  • Animal Models: Sexually immature female Han Wistar rats
  • Dosages: 5 and 25 mg/kg once daily
  • Administration: by oral gavage

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 442.47
Formula

C25H25F3N2O2

CAS No. 1639042-08-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1CC2=C(C(N1CC(C)(C)F)C3=C(C=C(C=C3F)C=CC(=O)O)F)NC4=CC=CC=C24

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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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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03236974 Completed Drug: Standard Arm - Fulvestrant|Drug: AZD9496 Postmenopausal Women With ER+ HER2- Primary Breast Cancer AstraZeneca October 5 2017 Phase 1
NCT02248090 Completed Drug: AZD9496 ER+ HER2- Advanced Breast Cancer AstraZeneca October 22 2014 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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