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AZD9496

Catalog No. T3975 CAS 1639042-08-2

AZD9496 is an orally available selective estrogen receptor(ERα) antagonist, with potential antineoplastic activity.

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AZD9496, CAS 1639042-08-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 51.00
2 mg	In stock	$ 71.00
5 mg	In stock	$ 118.00
10 mg	In stock	$ 198.00
25 mg	In stock	$ 370.00
50 mg	In stock	$ 548.00
100 mg	In stock	$ 792.00
1 mL * 10 mM (in DMSO)	In stock	$ 113.00

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Purity: 98.47%

Purity: 98.28%

Purity: 98.21%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	AZD9496 is an orally available selective estrogen receptor(ERα) antagonist, with potential antineoplastic activity.
Targets&IC50	ERα:0.28 nM.
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 Clinicalal trial[1].
Cell Research	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)

Molecular Weight	442.47
Formula	C25H25F3N2O2
CAS No.	1639042-08-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 82 mg/mL (185.3 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 82 mg/mL (185.3 mM)

References and Literature

1. Weir HM, et al. Cancer Res. 2016, 76(11):3307-18.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Ovarian Cancer Compound Library Bioactive Compound Library Bioactive Compounds Library Max Anti-Aging Compound Library Orally Active Compound Library

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Related compounds with same targets

Erteberel Bazedoxifene acetate Bazedoxifene hydrochloride Chrysin Estrogen receptor modulator 8 ARV-471 Liquiritigenin 4-hydroxyestrone-4-methyl ether

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Keywords

AZD9496 1639042-08-2 Endocrinology/Hormones Estrogen/progestogen Receptor Estrogen Receptor/ERR AZD 9496 AZD-9496 inhibit Inhibitor inhibitor

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