A SERD; binds to ERα and ERβ (IC50s = 6.1 and 8.8 nM

ARN810 – 25 mg

Brand:
Cayman
CAS:
1365888-06-7
Storage:
-20
UN-No:
Non-Hazardous - /

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.  

 

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SKU: 29595 - 25 mg Category:

Description

A SERD; binds to ERα and ERβ (IC50s = 6.1 and 8.8 nM, respectively); induces degradation of ERα in MCF-7 cells (EC50 = 0.7 nM); inhibits 17β-estradiol-induced ERα transcriptional activity in a reporter assay and reduces MCF-7 breast cancer cell viability (IC50 = 2 nM); inhibits 17β-estradiol-induced uterine weight gain in rats at 1 mg/kg; reduces tumor volume in tamoxifen-sensitive and -resistant MCF-7 mouse xenograft models

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

Synonyms:  GDC-0810|RG-6046

Molecular weight: 446.9

CAS: 1365888-06-7

Purity: ≥98%

Formulation: A solid

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