An indole-based SERM that binds to both ERα (IC50 = 26 nM) and ERβ (IC50 = 99 nM); antagonizes 17β-estradiol-dependent and hormone-independent growth of breast cancer cell proliferation (80% reduction with 10 nM) in a manner related to cell cycle arrest and downregulation of cyclin D1 and ERα

Bazedoxifene (acetate) – 10 mg

Brand:
Cayman
CAS:
198481-33-3
Storage:
-20
UN-No:
Non-Hazardous - /

Bazedoxifene (acetate) is a third generation selective estrogen receptor modulator (SERM). It is an indole-based ER ligand that binds to both ERα (IC50 = 26 nM) and ERβ (IC50 = 99 nM).{22645} Bazedoxifene (actetate) antagonizes 17β-estradiol-dependent MCF-7 and T47D breast cancer cell proliferation in vitro as well as hormone-independent growth of MCF-7:5C cells that are resistant to long-term estrogen deprivation (80% reduction with 10 nM).{22646} It has been shown to arrest cell cycling by downregulating cyclin D1 and ERα.{22646}  

 

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Description

An indole-based SERM that binds to both ERα (IC50 = 26 nM) and ERβ (IC50 = 99 nM); antagonizes 17β-estradiol-dependent and hormone-independent growth of breast cancer cell proliferation (80% reduction with 10 nM) in a manner related to cell cycle arrest and downregulation of cyclin D1 and ERα

Formal name: 1-[[4-[2-(hexahydro-1H-azepin-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol, acetate

Synonyms:  TSE 424

Molecular weight: 530.7

CAS: 198481-33-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Allosteric Modulators||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cancer|Cell Cycle||Research Area|Cell Biology|Cell Cycle||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Estrogens & Progestins

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