BSJ-03-204 triTFA is a potent and selective Cereblon- and CDK-targeted PROTAC (PROteolysis TArgeting Chimera) featuring Palbociclib-based ligands for the degradation of CDK4/6. It exhibits IC50 values of 26.9 nM for CDK4/D1 and 10.4 nM for CDK6/D1, indicating strong inhibitory capabilities. Notably, it spares IKZF1/3 from degradation and possesses anti-cancer activity [1].

BSJ-03-204 triTFA, at concentrations ranging from 0.0001 to 100 μM administered for 3 or 4 days, exhibits potent anti-proliferative effects on MCL cell lines [1]. Additionally, a 1 μM dose for 1 day strongly induces G1 phase arrest [1]. When applied at 0.1 to 5 μM for a period of 4 hours, BSJ-03-204 triTFA selectively leads to the degradation of CDK4/6 in WT cells without affecting IKZF1/3 [1].