AZD9496

AZD9496 is an effective, selective estrogen receptor (ERα) antagonist with an IC50 of 0.28 nM. AZD9496 is an orally active, selective estrogen receptor degrader (SERD) .

Product Specifications

CAS Number

[1639042-08-2]

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

Estrogen Receptor/ERR

Type

Reference compound

Related Pathways

Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/AZD9496.html

Purity

99.28

Solubility

DMSO : ≥ 104.5 mg/mL

Smiles

O=C(O)/C=C/C1=CC(F)=C([C@H]2N(CC(C)(F)C)[C@H](C)CC3=C2NC4=C3C=CC=C4)C(F)=C1

Molecular Formula

C25H25F3N2O2

Molecular Weight

442.47

Precautions

H315, H319, H335

References & Citations

[1]Weir HM, et al. AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and ESR1-Mutant Breast Tumors in Preclinical Models. Cancer Res. 2016 Jun 1;76 (11) :3307-18.|[2]De Savi C, et al. Optimization of a Novel Binding Motif to (E) -3- (3,5-Difluoro-4- ((1R,3R) -2- (2-fluoro-2-methylpropyl) -3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl) phenyl) acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist. J Med Chem. 2015 Oct 22;58 (20) :8128-40.|[3]Gough SM, et al. Oral Estrogen Receptor PROTAC Vepdegestrant (ARV-471) Is Highly Efficacious as Monotherapy and in Combination with CDK4/6 or PI3K/mTOR Pathway Inhibitors in Preclinical ER+ Breast Cancer Models. Clin Cancer Res. 2024 Aug 15;30 (16) :3549-3563.