PROTACs BTK Degrader-1 is a potent, selective and orally active PROTACs BTK degrader with an IC50 value of 34.51 nM and 64.56 nM for BTK WT and BTK-481S, respectively. PROTACs BTK Degrader-1 effectively reduces BTK protein levels and suppresses tumor growth. PROTACs BTK Degrader-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.