PROTAC AR Degrader-8 - CAS 3044108-04-2

PROTAC AR Degrader-8 (Compound NP18) functions as a PROTAC degrader targeting the androgen receptor (AR) and effectively degrades AR-FL in both 22Rv1 and LNCaP cells with DC50 values of 0.018 μM and 0.14 μM, respectively. It also degrades AR-V7 in 22Rv1 cells with a DC50 of 0.026 μM. Additionally, PROTAC AR Degrader-8 inhibits the proliferation of 22Rv1 and LNCaP cancer cells, exhibiting IC50 values of 0.038 μM and 1.11 μM. It induces cell cycle arrest at the G2/M phase and triggers apoptosis in 22Rv1 cells (apoptosis) . Demonstrating anticancer efficacy, PROTAC AR Degrader-8 shows activity in both mouse and zebrafish models. [Pink: ligand for target protein AR ligand-33; Black: linker; Blue: ligand for E3 ligase Cereblon]

Androgen Receptor, Apoptosis, PROTACs

PROTAC, Endocrinology/Hormones, Apoptosis

3044108-04-2

C40H41N5O7

703.783

O=C1C=2C=CC=C(NCCOC3=CC=C(C=C3)C(C4=CC=C(OCC5=NC(=CC=C5)N6CCOCC6)C=C4)(C)C)C2C(=O)N1C7C(=O)NC(=O)CC7

-20°C

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