ARN810

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ARN810

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Cat No: 29595

Biochemicals - More Biochemicals

ARN810 is a selective estrogen receptor degrader (SERD) that binds to ERα and ERβ (IC50s = 6.1 and 8.8 nM, respectively) and induces degradation of ERα in MCF-7 cells (EC50 = 0.7 nM).{53182} It inhibits ERα transcriptional activity induced by 17β-estr...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

(2E)-3-[4-[(1E)-2-(2-chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)-1-buten-1-yl]phenyl]-2-propenoic acid

Correlated keywords:

ARN-810 Brilanestrant GDC0810 RG6046 RO-7056118 RO7056118 ER-? ? MCF7

Product Overview:
ARN810 is a selective estrogen receptor degrader (SERD) that binds to ERα and ERβ (IC50s = 6.1 and 8.8 nM, respectively) and induces degradation of ERα in MCF-7 cells (EC50 = 0.7 nM).{53182} It inhibits ERα transcriptional activity induced by 17β-estradiol (Item No. 10006315) in a reporter assay and reduces MCF-7 breast cancer cell viability (IC50 = 2 nM). ARN810 (1 mg/kg, p.o.) inhibits 17β-estradiol-induced uterine weight gain in rats. It reduces tumor volume in tamoxifen-sensitive and -resistant MCF-7 mouse xenograft models in a dose-dependent manner.

Size	1 mg
Shipping	dry ice
CAS Number	1365888-06-7
Molecular Formula	C₂₆H₂₀ClFN₂O₂
SMILES	ClC1=C(/C(CC)=C(C2=CC=C(/C=C/C(O)=O)C=C2)/C3=CC(C=NN4)=C4C=C3)C=CC(F)=C1
Molecular Weight	446,9
Formulation	A solid
Purity	≥98%
Custom Code	2933.99
UNSPSC code	12352100

Technical File

MSDS

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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.