Amino-PEG3-C2-Azido 

Amino-PEG3-C2-Azido is a PEG-based PROTAC linker can be used in the synthesis of the PARP1 degrader iRucaparib-TP3 (HY-130645)^[1]. Amino-PEG3-C2-Azido 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.

Pomalidomide (a CRBN ligand and a known immunomodulatory imide drug (IMiD)) is conjugated to Rucaparib through a tri(ethylene glycol) (PEG3) linker to afford a compound that we designate as iRucaparib-TP3 (IMiD-Rucaparib with a triazole-PEG3 linker). iRucaparib-TP3 induces PARP1 degradation^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

218.25

C₈H₁₈N₄O₃

134179-38-7

Liquid

Colorless to light yellow

[N-]=[N+]=NCCOCCOCCOCCN

Room temperature in continental US; may vary elsewhere.

-20°C, protect from light, stored under nitrogen

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

• [1]. Wang S, et al. Uncoupling of PARP1 trapping and inhibition using selective PARP1 degradation. Nat Chem Biol. 2019 Dec;15(12):1223-1231.  [Content Brief]