PROTAC BRD4 Degrader-13

PROTAC BRD4 Degrader-13 (compound 9d) is a von Hippel-Lindau system-based PROTAC BRD4 degrader with a linker that can be coupled to ADC antibodies to form PACs (PROTAC-antibody Conjugates). PROTAC BRD4 Degrader-13 can be coupled to STEAP1 and CLL1 antibodies to degrade BRD4 protein in PC3 prostate cancer cells with DC50 values ​​of 0.025 nM and 6.0 nM, respectively[1].

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[1]Dragovich PS, et, al. Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy. J Med Chem. 2021 Mar 11;64(5):2576-2607.