A SERD (IC50 = 0.138 nM for ERα downregulation); selective for ERα compared to other nuclear hormone receptors (IC50s = 0.0008

AZD 9496 – 5 mg

Brand:
Cayman
CAS:
1639042-08-2
Storage:
-20
UN-No:
De Minimis - 3077 / 9

AZD 9496 is a potent and selective estrogen receptor downregulator (SERD) with an IC50 value of 0.138 nM for estrogen receptor α (ERα) downregulation.{39174} It is selective for ERα compared to other nuclear hormone receptors with IC50 values of 0.0008, 0.54, 9.2, and 30 μM for ERα, progesterone receptor (PR), glucocorticoid receptor (GR), and androgen receptor (AR), respectively. AZD 9496 decreases ERα activity (IC50 = 0.282 nM), measured via quantification of downstream PR activity, and reduces proliferation of MCF-7 breast cancer cells (IC50 = 0.0398 nM). It also inhibits MCF-7 xenograft growth in mice in a dose-dependent manner. AZD 9496 is orally bioavailable and formulations containing it are under investigation in clinical trials for treatment of ER positive breast cancer.  

 

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Description

A SERD (IC50 = 0.138 nM for ERα downregulation); selective for ERα compared to other nuclear hormone receptors (IC50s = 0.0008, 0.54, 0.92, and 30 μM for ERα, PR, GR, and AR, respectively); decreases ERα activity (IC50 = 0.282 nM for PR antagonism); reduces proliferation of MCF-7 breast cancer cells (IC50 = 0.0398 nM); inhibits MCF-7 xenograft growth in mice in a dose-dependent manner,

Formal name: (2E)-3-[3,5-difluoro-4-[(1R,3R)-2-(2-fluoro-2-methylpropyl)-2,3,4,9-tetrahydro-3-methyl-1H-pyrido[3,4-b]indol-1-yl]phenyl]-2-propenoic acid

Synonyms: 

Molecular weight: 442.5

CAS: 1639042-08-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cancer||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Estrogens & Progestins

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