Dual PI3Kδ/γ Inhibition By RP6530 Induces Apoptosis and Cytotoxicity In B-Lymphoma Cells
Vakkalanka S, Viswanadha S, Gaudio E et al.
Key Points:
Study explored therapeutic potential of RP6530(PI3Kδ/γ inhibitor) in B-cell lymphomas.
Authors demonstrated high potency of RP6530 against PI3Kδ (IC50=24.5 nM) and γ (IC50=33.2 nM) enzymes with selectivity over α (>300-fold) and β (>100-fold) isoforms.
RP6530 caused growth inhibition of lymphoma cell lines (OCI-LY-1, OCI-LY-10, Raji, TOLEDO, KG-1, JEKO, REC-1).
Use of RP6530 on patient-derived primary cells caused increase in cell death.
Implications:
- RP6530 is dual PI3Kδ/γ inhibitor that inhibited growth of B-cell lymphoma cell lines and in panel of lymphoma primary cells.
View the original abstract on the ASH website.
