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ARN-509

Cat No.
CEI-1217
Description
ARN-509 is a selective and competitive inhibitor of androgen receptor with an IC50 value of 16 nM.
Product Overview
ARN-509, a synthetic biaryl thiohydantoin compound, is a competitive androgen receptor (AR) inhibitor and fully antagonistic to AR overexpression. The IC50 of ARN-509 is 16 nmol/L. AR, included in the steroid receptor superfamily, is important for prostate cell proliferation and male sexual differentiation. AR overexpression is a common and important feature of castration resistant prostate cancer (CRPC). ARN-509 (1 μmol/L) treatment for 48 hours resulted in increased DNA damage in LNCaP cells, LNCaP-AR cells and VCaP cells. In LNCaP cell line, treatment with ARN-509 (1 μmol/L) resulted in decreased cell survival. Treatment with ARN-509 (1 μmol/L) for 48 hours significantly decreased C-NHEJ-mediated recombination (>60%) in LNCaP cells that had been transfected with V(D)J recombination substrate along with RAG1 and RAG2 expression vectors. ARN-509 showed robust transcriptional and proliferative agonist activity in AR F876L-expressing cells, and promoted AR DNA binding in LNCaP/SRα F876L cells. Orally treated with ARN-509 (10 mg/kg/d) for 17 days, androgendriven luciferase reporter-gene activity in castrate male immunodeficient mice harboring LNCaP/AR-luc xenograft tumors (coexpressing exogenous AR and the AR-dependent reporter ARR2-Pb-luc), was consistently reduced. This indicated that ARN-509 inhibited AR in vivo. ARN-509 made tumors exhibit a decrease in proliferative index and an increase in apoptotic rate.
CAS No.
956104-40-8
Molecular Weight
477.43
Purity
0.98
Storage
Store at -20°C
Synonyms
ARN 509; ARN509
Targets
Androgen Receptor; GABAA receptor
IC50
16 nM; 3 μM
Molecular Formula
C21H15F4N5O2S
Chemical Name
4-[7-[6-cyano-5-(trifluoromethyl)pyridin-3-yl]-8-oxo-6-sulfanylidene-5,7-diazaspiro[3.4]octan-5-yl]-2-fluoro-N-methylbenzamide
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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