AR-V7 Degrader

MTX-23 is a PROTAC degrader targeting androgen receptor splice variant 7 (AR-V7) and full-length androgen receptor (AR-FL), with DC₅₀ values of 0.37 μM and 2 μM, respectively. MTX-23 binds to the DNA-binding domains of AR-V7 and AR-FL, recruits the VHL E3 ubiquitin ligase (E3 ubiquitin ligase) and induces their degradation. MTX-23 reduces the proliferation of prostate cancer cells, promotes their apoptosis (apoptosis), and also inhibits tumor growth in mouse models. MTX-23 can be used for the research of prostate cancer.

PROTAC AR-V7 degrader-1 is a selective AR-V7 degrader with a DC₅₀ of 0.32 μM. PROTAC AR-V7 degrader-1 inhibits cancer cell proliferation. PROTAC AR-V7 degrader-1 is applicable to the research of castration-resistant prostate cancer.

TD-802 is a CRBN-recruiting PROTAC androgen receptor (AR) degrader with liver microsomal stability and in vivo pharmacokinetic properties. TD-802 exhibits weak degrading activity against the AR-V7 splice variant, and its degradation process depends on the ubiquitin-proteasome system and Cullin-Ring ubiquitin ligase. TD-802 inhibits the proliferation of AR-dependent prostate cancer cells and the growth of AR-positive prostate cancer tumors in in vivo xenograft models.