FDU73

FDU73 (Compound 27) (0.01 nM-1 μM; 1-24 h) potently induces concentration- and time-dependent degradation of BTK in JeKo-1 cells, with a DC₅₀ of 2.9 nM, and achieves complete degradation at a concentration of 100 nM after 4 h of treatment^[1].
FDU73 (0.1 nM-1 μM; 24 h) potently induces concentration-dependent degradation of wild-type and BTK^C481S mutant BTK in TMD8 cells, with DC₅₀ values of 2.8 nM and 4.3 nM, respectively^[1].
FDU73 (10 nM; 24 h) induces BTK degradation in JeKo-1 cells via the ubiquitin-proteasome system in a CRBN- and proteasome-dependent manner^[1].
FDU73 (0.1 nM-1 μM; 8 h) selectively induces BTK degradation in JeKo-1 cells without affecting the novel CRBN substrates IKZF1, IKZF3 or GSPT1^[1].
FDU73 (100 nM; 4 h) exhibits proteome-wide selectivity for BTK degradation in JeKo-1 cells, with only BTK, CSK and BLK showing significant downregulation at 100 nM for 4 h^[1].
FDU73 potently inhibits the proliferation of TMD8 BTK^WT cells with an IC₅₀ of 9.9 nM, and also exhibits potent activity against TMD8 BTK^C481S mutant cells^[1].

FDU73 exhibits excellent metabolic stability in mouse liver microsomes, with a half-life of over 145 min^[1].