bsj 03 204

BSJ-03-204 is a rationally designed PROTAC composed of cereblon and CDK ligands that functions as a potent and selective palbociclib-based CDK4/6 dual degrader, achieving nanomolar inhibition of CDK4/D1 and CDK6/D1 complexes without inducing IKZF1/3 degradation, BSJ-03-204 exhibit strong anticancer activity with improved selectivity.

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].

Palbociclib-C4-Boc is a target protein ligand-linker conjugate composed of the CDK4/6 ligand Palbociclib and a PROTAC linker, capable of recruiting E3 ligase. It is utilized in the synthesis of PROTACBSJ-03-204.