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.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, protect from light, stored under nitrogen)
Scientific Category
Reference compound1
Clinical Information
Phase 1
Available Sizes
Frequently Asked Questions
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