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AR antagonist 10

CAT: 0804-HY-170951Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-170951Size:1 Each
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Description
AR antagonist 10 (Compound Y5) is potent and orally active androgen receptor (AR) antagonist with an IC50 of 0.04 μM. AR antagonist 10 demonstrates dual mechanisms of action, antagonizes AR by disrupting AR dimerization, and induces AR degradation via the ubiquitin-proteasome pathway. AR antagonist 10 exhibits excellent activity against variant drug-resistant AR mutants. AR antagonist 10 effectively suppresses the tumor growth of the LNCaP xenograft. AR antagonist 10 is potential to be used for drug-resistant prostate cancer[1].
CAS Number
3068489-78-8
UNSPSC
12352005
Target
Androgen Receptor
Related Pathways
Vitamin D Related/Nuclear Receptor
Field of Research
Cancer
Smiles
O=C(C1=CC2=C(OC=C1)C=CC(Cl)=C2)NC3=NC(CN4CCOCC4)=NS3
Molecular Formula
C18H17ClN4O3S
Molecular Weight
404.87
References & Citations
[1]Jianing Liao, et al. Discovery of N‑ (1,2,4-Thiadiazol-5-yl) benzo[b]oxepine-4-carboxamide Derivatives as Novel Antiresistance Androgen Receptor Antagonists. Journal of Medicinal Chemistry 2025 68 (3), 3445-3459.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported

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