AR antagonist 9
AR antagonist 9
SKU:QM-0152854
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Product Details
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Description
AR antagonist 9 is an orally bioavailable selective androgen receptor (AR) antagonist that exerts anticancer effects by disrupting the dimerization of AR ligand-binding domains, showing potential for overcoming drug resistance in prostate cancer (PCa). Its AR antagonistic activity has an IC50 value of 0.051 μM, comparable to Enzalutamide (IC50 = 0.060 μM). AR antagonist 9 demonstrated superior efficacy against ARF876L/T877A and ARW741C mutants compared to Enzalutamide (HY-70002). Furthermore, AR antagonist 9 exhibited favorable pharmacokinetic properties, with an oral bioavailability of F = 66.24% in rats. In the LNCaP xenograft mouse model, oral administration of AR antagonist 9 significantly inhibited tumor growth. AR antagonist 9 holds promise for research into overcoming PCa drug resistance[1].
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Molecular Formula
C18H13F4NO2
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Molecular Weight
351.29
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Smiles
O=C1C=C(C(F)(F)F)C2=C(O1)C=C(N(CC3=CC=C(F)C=C3)C)C=C2
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Target
Androgen Receptor
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Shipping Conditions
Room temperature
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AR antagonist 9
AR antagonist 9 is a premium-grade research compound supplied by Quantimol for laboratory and scientific applications.