ZNU-IMB-Z15 

ZNU-IMB-Z15 (Compound Z15) is an antagonist of the androgen receptor (AR) and also a selective degrader of AR and ARV7. ZNU-IMB-Z15 can directly bind to the ligand-binding domain (LBD) and activation function-1 region of AR, and promote AR degradation through the proteasome pathway. ZNU-IMB-Z15 effectively inhibits the transcriptional activity of AR, AR mutants, and AR splice variants (ARVs), downregulating the mRNA and protein levels of AR downstream target genes, thereby overcoming the resistance to second-generation antiandrogen drugs induced by AR LBD mutations, AR amplification, and ARVs in castration-resistant prostate cancer (CRPC). ZNU-IMB-Z15 can inhibit the proliferation of AR-positive CRPC cell lines and induce their apoptosis, demonstrating anticancer activity both in vivo and in vitro^[1].

411.50

C₂₀H₁₇N₃O₃S₂

920915-26-0

O=C(NC1=NC(C2=CC=CS2)=CS1)C3=CC=C(OCC4=C(C)ON=C4C)C=C3

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Wu M, et al. Selective androgen receptor degrader (SARD) to overcome antiandrogen resistance in castration-resistant prostate cancer[J]. Elife, 2023, 12: e70700.  [Content Brief]