Description
A potent, selective, and irreversible BTK inhibitor with IC50 of 7nM; inhibits BTK kinase activity with an IC50 of 7nM, inhibits autophosphorylation of BTK on Tyr223 in cells with an EC50 of 475nM, and inhibits phosphorylation of a downstream effector PLCgamma2 (Tyr759) with an EC50 of 318nM; induces a G1 cell cycle arrest that is associated with pronounced degradation of BTK protein in Ramos cells; inhibits the proliferation of B-cell lymphoma cancer cell lines at submicromolar concentrations. Blood Cancer Preclinical