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AR antagonist 9

CAT: 0804-HY-159922Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-159922Size:1 Each
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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].
UNSPSC
12352101
Target
Androgen Receptor
Type
Reference compound
Related Pathways
Vitamin D Related/Nuclear Receptor
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/ar-antagonist-9.html
Smiles
O=C1C=C(C(F)(F)F)C2=C(O1)C=C(N(CC3=CC=C(F)C=C3)C)C=C2
Molecular Formula
C18H13F4NO2
Molecular Weight
351.29
References & Citations
[1]Liao J, et al. Identification of Oral Bioavailable Coumarin Derivatives as Potential AR Antagonists Targeting Prostate Cancer. J Med Chem. 2024 Nov 14;67 (21) :19395-19416.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported

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