Home Endocrinology & Hormones Estrogen/progestogen Receptor inhibitor AZD9496 For research use only.

AZD9496

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

AZD9496 Chemical Structure

CAS No. 1639042-08-2

Purity & Quality Control

Batch: S837201 DMSO]88 mg/mL]false]Ethanol]88 mg/mL]false]Water]Insoluble]false Purity: 99.78%
99.78

AZD9496 Related Products

Signaling Pathway

Estrogen/progestogen Receptor Signaling Pathways

Estrogen/progestogen Receptor Signaling Pathway

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
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].
Cell Research 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 for the time indicated.
In Vivo
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.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].
Animal Research Animal Models Sexually immature female Han Wistar rats
Dosages 5 and 25 mg/kg once daily
Administration by oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03236974 Completed
Postmenopausal Women With ER+ HER2- Primary Breast Cancer
AstraZeneca
 October 5 2017 Phase 1
NCT02248090 Completed
ER+ HER2- Advanced Breast Cancer
AstraZeneca
 October 22 2014 Phase 1

Chemical Information & Solubility

Molecular Weight 442.47 Formula

C25H25F3N2O2
CAS No. 1639042-08-2 SDF Download AZD9496 SDF
Smiles CC1CC2=C(C(N1CC(C)(C)F)C3=C(C=C(C=C3F)C=CC(=O)O)F)NC4=CC=CC=C24
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 88 mg/mL ( (198.88 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 88 mg/mL

Water : Insoluble


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In vivo
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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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