AZD9496 (maleate)

AZD9496 maleate is a potent and selective estrogen receptor (ERα) antagonist with IC50 of 0.28 nM. AZD9496 maleate is an orally bioavailable selective oestrogen receptor degrader (SERD) .

Product Specifications

CAS Number

[1639042-28-6]

UNSPSC

12352005

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-maleate.html

Concentration

10mM

Purity

99.35

Solubility

DMSO : ≥ 100 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.O=C(O)/C=C\C(O)=O

Molecular Formula

C29H29F3N2O6

Molecular Weight

558.55

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.