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AR antagonist BG-15a

Chemical Structure : AR antagonist BG-15a

CAS No.:

AR antagonist BG-15a

Catalog No.: PC-23464Not For Human Use, Lab Use Only.

AR antagonist BG-15a is a novel small molecule androgen receptor (AR) antagonist, binds to the ligand-binding domain of AR, promotes AR localization to the nucleus, yet potently and selectively down-regulates AR-target genes.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

AR antagonist BG-15a is a novel small molecule androgen receptor (AR) antagonist, binds to the ligand-binding domain of AR, promotes AR localization to the nucleus, yet potently and selectively down-regulates AR-target genes.
BG-15a elicits a decrease in cell and tumor growth in vitro and in vivo in models of mCRPC.
BG-15a treatment causes the collapse of chromatin loops between enhancers and promoters at key genes in the AR-driven epigenome.

Physicochemical Properties

M.Wt 471.46
Formula C21H16F3N7OS
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-(3-(4-(1H-1,2,3-triazol-4-yl)benzyl)-4,4-dimethyl-5-oxo-2-thioxoimidazolidin-1-yl)-3-(trifluoromethyl)picolinonitrile

References

1. Kohrt SE, et al. Proc Natl Acad Sci U S A. 2024 Nov 26;121(48):e2406239121.

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