Home Endocrinology & Hormones Estrogen/progestogen Receptor inhibitor AZD9496

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AZD9496 Estrogen/progestogen Receptor inhibitor

Cat.No.S8372

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

Chemical Structure

Molecular Weight: 442.47

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Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 442.47 Formula

C25H25F3N2O2

 Storage (From the date of receipt)
CAS No. 1639042-08-2 Download SDF Storage of Stock Solutions

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

Solubility

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

Molarity Calculator

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In vivo
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Mechanism of Action

Targets/IC50/Ki
estrogen receptor [1]
In vitro

AZD9496 showed pmol/L equipotent binding to both ERα and ERβ isoforms. This compound 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 this chemical 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. This compound is a potent, oral inhibitor of breast tumor growth in vivo. It 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. This chemical is currently being evaluated in a phase I clinical trial[1].
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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