Palbociclib-propargyl  (Synonyms: PROTAC CDK6 ligand 1)

Palbociclib-propargyl is a ligand for target protein CDK6 for PROTAC, and binds to CRBN ligand via a PEG linker to make a PROTAC CP-10. CP-10 shows a DC₅₀ of 2.1 nM for CDK6^[1]. Palbociclib-propargyl is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

485.58

C₂₇H₃₁N₇O₂

2366269-23-8

Solid

Light yellow to yellow

O=C1C(C(C)=O)=C(C)C2=CN=C(NC3=NC=C(N4CCN(CC#C)CC4)C=C3)N=C2N1C5CCCC5

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)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Su S, et al. Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders. J Med Chem. 2019 Aug 22;62(16):7575-7582.  [Content Brief]