ZZ151 (ZZ-151) is a highly potent and selective SOS1 degrader PROTAC with DC50 of 15.7 nM (Dmax=100%).
ZZ151 induces SOS1 degradation via the VHL-dependent proteasomal degradation pathway.
ZZ151 potently, specifically and quickly induces SOS1 degradation.
ZZ151 potently induces SOS1 degradation in cells harboring KRAS mutations of G12C, G12D, G12V, G12R, G12S, and G13D with DC50 values ranged from 8.41 to 41.4 nM.
ZZ151 (20 mg/kg) significantly inhibits the tumor growth of KRASG12D- and KRASG12V-mutant xenografts in mice, with no body weight loss.
