Catalog No.: PC-38047Not For Human Use, Lab Use Only.
Bavdegalutamide (ARV-110) is an orally bioavailable, specific androgen receptor (AR) PROTAC degrader that leads to ubiquitination and degradation of AR with DC50 of <1 nM.
Bavdegalutamide (ARV-110) is an orally bioavailable, specific androgen receptor (AR) PROTAC degrader that leads to ubiquitination and degradation of AR with DC50 of <1 nM.
At the dose of 0.01 nM-300 nM, ARV-110 leads to AR degradation in LNCaP cells in a dose-dependent manner.
In VCaP cells, ARV-110 leads to AR degradation in a time-dependent manner.
ARV-110 suppresses the expression of the AR-target gene PSA. ARV-110 inhibits AR-dependent cell proliferation and induces apoptosis at low nanomolar concentrations.
ARV-110 degrades clinically relevant mutant AR proteins (WT AR, F876L, T877A, M896V, and H874V). retains activity even in a high androgen environment (R1881, 100 nM) in VCaP cells.
ARV-110 exhibits a greater than 90% AR degradation in LNCaP, VCaP, and prostate cancer PDX models.
ARV-110 exhibits significant inhibition of tumor growth and AR signaling in vivo.
