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AR Degrader-3

CAT: 0804-HY-178938Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-178938Size:1 Each
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
AR Degrader-3 is an orally active molecular glue that targets AR/ARV7 and induces the degradation of AR and ARV7 through the ubiquitin-proteasome pathway (UPP). AR Degrader-3 directly interacts with the ligand-binding domain (LBD) and the N-terminal domain (NTD) of AR. AR Degrader-3 effectively suppresses the transcriptional activity of wild-type AR (AR-WT), AR mutants, and ARV7. AR Degrader-3 downregulates the mRNA and protein levels of downstream AR target genes, thereby overcoming antiandrogen resistance mediated by ARV7 and AR point mutations. AR Degrader-3 induces apoptosis in Enzalutamide (ENZa) -resistant cells and increases cleaved caspase-3 protein levels. AR Degrader-3 can be used for the study of castration-resistant prostate cancer (CRPC).
CAS Number
1182011-65-9
UNSPSC
12352005
Target
Androgen Receptor; Apoptosis; Caspase; Molecular Glues
Related Pathways
Apoptosis; PROTAC; Vitamin D Related/Nuclear Receptor
Field of Research
Cancer; Endocrinology
Smiles
CC1=NOC(C)=C1COC2=CC=C(C(NC3=NC(C4=CC=C(OC)C=C4)=CS3)=O)C=C2
Molecular Formula
C23H21N3O4S
Molecular Weight
435.50
References & Citations
[1]Zhang R, et al. Development of dual AR/ARV7 degraders with 3,5-dimethylisoxazole to overcome antiandrogen resistance in castration-resistant prostate cancer. Eur J Med Chem. 2026 Jan 5;301:118259.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
Caspase 3

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