CP-10 is a PROTAC with highly selective and remarkable CDK6 degradation (DC50: 2.1 nM). It inhibits the proliferation of several hematopoietic cancer cells including multiple myeloma and can degrade mutated and overexpressed CDK6.
Pomalidomide-PEG1-C2-N3 is a compound that has been synthesized as a conjugate of an E3 ligase ligand-linker. This compound incorporates the cereblon ligand based on Pomalidomide and a 1-unit PEG linker, which are commonly used in PROTAC technology. Utilizing Pomalidomide-PEG1-C2-N3, it is possible to design a selective CDK6 PROTAC degrader known as CP-10. CP-10 effectively induces the degradation of CDK6, displaying a DC50 value of 2.1 nM[1].
Palbociclib-propargyl, a PROTAC ligand targeting the protein CDK6, connects to the CRBN ligand through a PEG linker to form PROTAC CP-10. CP-10 exhibits a potent DC50 value of 2.1 nM against CDK6[1].