Pomalidomide-PEG1-C2-N3  (Synonyms: Cereblon Ligand-Linker Conjugates 13; E3 ligase Ligand-Linker Conjugates 50)

Pomalidomide-PEG1-C2-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 1-unit PEG linker used in PROTAC technology. Pomalidomide-PEG1-C2-N3 can be used to design a selective CDK6 PROTAC degrader CP-10. CP-10 induces the degradation of CDK6 with an DC₅₀ of 2.1 nM^[1]. Pomalidomide-PEG1-C2-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.

386.36

C₁₇H₁₈N₆O₅

2271036-44-1

Solid

Light yellow to yellow

O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC=C3NCCOCCN=[N+]=[N-])=O

Room temperature in continental US; may vary elsewhere.

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

• [1]. Su S, et al. Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders. J Med Chem. 2019 Aug 2.  [Content Brief]