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Catalog No.S8372

2 publications

AZD9496 Chemical Structure

CAS No. 1639042-08-2

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

Selleck's AZD9496 has been cited by 2 publications

1 Customer Review

  • Kaempferol and ER /PR inhibitor suppress the migration and Rho activity of MCF-7 cells. Notes: (A) MCF-7 ER +/PR+ breast cancer cells were allowed to migrate in response to 20 μmol/L kaempferol and/or 0.1 nmol/L AZD9496 (ER inhibitor) and 200 μmol/L megestrol acetate (PR inhibitor) for 6 h. Results are presented as mean ± SD of 5 independent experiments. (B, C) MCF-7 cells were incubated with 20 μmol/L kaempferol and/or 0.1 nmol/L AZD9496 and 200 μmol/L MA for 1 h, and then subjected to the RhoA (B) and Rac1 (C) activity assays. The relative levels of Rho activity were normalized to the average value of controls. Results are presented as mean ± SD of 3 independent experiments. Abbreviations: AZD, AZD9496; Ctrl, control; ER, estrogen receptor; MA, megestrol acetate; ns, no significance; PR, progesterone receptor.

    Onco Targets Ther, 2017, 10: 4809–4819 . AZD9496 purchased from Selleck.

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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.
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].


Cell Research:[1]
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  • 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.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Sexually immature female Han Wistar rats
  • Dosages: 5 and 25 mg/kg once daily
  • Administration: by oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 88 mg/mL (198.88 mM)
Ethanol 88 mg/mL (198.88 mM)
Water Insoluble

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Chemical Information

Molecular Weight 442.47


CAS No. 1639042-08-2
Storage powder
in solvent
Synonyms N/A
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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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

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Estrogen/progestogen Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID