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AR antagonist 9

Ref. TM-T203275

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Targetmol

Product Information

Name:AR antagonist 9
Brand:Targetmol
Description:AR antagonist 9 is an orally active, selective androgen receptor (AR) antagonist that inhibits cancer by disrupting the formation of AR ligand-binding domain dimers, showing potential in overcoming drug resistance in prostate cancer (PCa). Its antagonistic activity against AR has an IC50 of 0.051 μM, comparable to Enzalutamide (IC50= 0.060 μM). This compound demonstrates superior inhibitory effects on ARF876L/T877A and ARW741C mutants compared to Enzalutamide. Additionally, AR antagonist 9 possesses favorable pharmacokinetic properties, with an oral bioavailability (F) of 66.24% in rats, and significantly inhibits tumor growth in LNCaP xenograft mouse models upon oral administration. AR antagonist 9 holds promise for research in overcoming PCa resistance.
Notice:Our products are intended for lab use only. For any other use, please contact us.

Chemical properties

Molecular weight:351.29
Formula:C18H13F4NO2
Color/Form:Solid

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