Acolbifene

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Acolbifene

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Cat No: 23931

Biochemicals - Receptor Pharmacology

Acolbifene is a selective estrogen receptor modulator (SERM). It inhibits transcriptional activity of estrogen receptor α (ERα) and ERβ induced by estradiol (E2; Item No. 10006315; IC50s = 2 and 0.4 nM, respectively).{38866} It binds to ERs in cytosol...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

(2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidinyl)ethoxy]phenyl]-2H-1-benzopyran-7-ol

Correlated keywords:

SCH57068 EM652 ER-? ? noncancerous MCF7 ZR751 T-47-D em-652

Product Overview:
Acolbifene is a selective estrogen receptor modulator (SERM). It inhibits transcriptional activity of estrogen receptor α (ERα) and ERβ induced by estradiol (E2; Item No. 10006315; IC50s = 2 and 0.4 nM, respectively).{38866} It binds to ERs in cytosol from human breast cancer and non-cancerous uterine cells (Kis = 0.047 and 0.042 nM, respectively) and to ERs in cytosol from rat uterine cells (IC50 = 0.44 nM) but not to progesterone or androgen receptors in cytosol from rat uterine and ventral prostate cells (IC50s = 22,500 and >10,000 nM, respectively).{38866,38867} Acolbifene inhibits E2-stimulated proliferation of T47D, ZR-75-1, and MCF-7 breast cancer cells (IC50s = 0.146, 0.75, and 0.321 nM, respectively) but not basal proliferation.{38866} Acolbifene (50 μg per day) inhibits tumor growth stimulated by estrone (E1; Item No. 10006485) in a ZR-75-1 human breast cancer xenograft model in ovariectomized mice.{38868} It also inhibits E1-stimulated endometrial epithelium thickening in vivo in ovariectomized mice when administered at a dose of 50 μg per day.

Size	1 mg
Shipping	dry ice
CAS Number	182167-02-8
Molecular Formula	C₂₉H₃₁NO₄
SMILES	OC1=CC=C(C(C)=C(C2=CC=C(O)C=C2)[C@H](C3=CC=C(OCCN4CCCCC4)C=C3)O5)C5=C1
Molecular Weight	457,6
Formulation	A solid
Purity	≥98%
Custom Code	2933.39
UNSPSC code	12352100

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.