AS2541019 is a novel potent, selective, orally active PI3Kδ inhibitor with IC50 of 20.1 nM, >100-fold selectivity over other PI3K isoforms.
AS2541019 inhibits Akt phosphorylation in human Ramos B cell line with IC50 of 14.3 nM.
AS2541019 effectively inhibits anti-IgM stimulated B cell proliferation and human B cell proliferation with IC50 of 4.3 and 3.6 nM, respectively.
AS2541019 significantly inhibits both T-dependent and T-independent de novo antibody production in peripheral blood in vivo.
AS2541019 significantly prolongs graft survival time by inhibiting xenoreactive antibody production in rat concordant xenotransplant model.
