DFCI-002-06 is an orally active dual-target HCK/BTK PROTAC degrader with DC₅₀ values for HCK and BTK of 1.3 and 4.5 nM respectively. DFCI-002-06 retains higher anti-tumor activity than the HCK/BTK dual-target inhibitor, inducing apoptosis in cancer cells. DFCI-002-06 can be used for the study of MYD88 mutant B-cell malignancies [1]. (Pink: Src and Btk ligand; Blue: Cereblon ligand; Black: linker).
References:
[1]. Hatcher JM, et al. Discovery and Characterization of a First-In-Class HCK/BTK PROTAC DFCI-002-06 for the Treatment of MYD88 Mutated B Cell Malignancies. J Med Chem. 2026 Jan 22;69(2):1119-1134.
References:
[1]. Hatcher JM, et al. Discovery and Characterization of a First-In-Class HCK/BTK PROTAC DFCI-002-06 for the Treatment of MYD88 Mutated B Cell Malignancies. J Med Chem. 2026 Jan 22;69(2):1119-1134.