AZD9496

For research use only.

Catalog No.S8372

2 publications

AZD9496 Chemical Structure

Molecular Weight(MW): 442.47

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

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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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Choose Selective Estrogen/progestogen Receptor Inhibitors

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

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

* 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 442.47
Formula

C25H25F3N2O2

CAS No. 1639042-08-2
Storage powder
in solvent
Synonyms N/A
Smiles CC1CC2=C([NH]C3=CC=CC=C23)C(N1CC(C)(C)F)C4=C(F)C=C(\C=C\C(O)=O)C=C4F

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID