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AR antagonist 9

CAT: 0931-T203275-01Size: 10 mgDry Ice: NoHazardous: No
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CAT#:0931-T203275-01Size:10 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Target
Androgen Receptor
Related Pathways
Endocrinology/Hormones
Bioactivity
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.
Molecular Formula
C18H13F4NO2
Molecular Weight
351.29
Shipping Conditions
Ice Packs
Storage Temperature
-20°C

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