Propargyl-PEG1-acid, a PEG-based PROTAC linker, enables the synthesis of BTK-CRBN PROTACs, specifically Ibrutinib-based PROTAC 4 and PROTAC 5. At a concentration of 10 μM, PROTAC 5 facilitates the degradation of BTK and induces the degradation of CSK, LYN, and LAT2[1].
体外活性
BTK-CRBN PROTACs act as stoichiometric degraders, resulting in degradation of BTK protein. Degradation of BTK is a result of cereblon E3 ligases family recruitment[1].
存储条件
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.