Ibrutinib-MPEA

Ibrutinib-MPEA is an orally active, blood-brain barrier permeable inhibitor of BTK and STAT5. As a derivative of Ibrutinib (HY-10997) conjugated with a PROTAC linker, Ibrutinib-MPEA allows the synthesis of a series of PROTAC molecules. Ibrutinib-MPEA significantly reduces the proliferation of neoplastic mast cells and primary mastocytoma cells by inducing apoptosis and inhibiting IgE-dependent histamine release. Ibrutinib-MPEA is applicable to the research of canine mast cell tumors, cerebral ischemia/reperfusion injury in diabetic mice, and neuroinflammation-related diseases^[1][2][3]. In Vitro:Ibrutinib-MPEA serves as a conjugate of Btk ligand and linker for the synthesis of a series of PROTAC molecules, such as P13I. When applied to human Burkitt's lymphoma RAMOS cells, P13I degrades 73% and 89% of Btk at concentrations of 10 and 100 nM, respectively^[4].