LL-00084282 is a potent, selective and efficacious dual PI3Kδ/γ inhibitor with IC50 of 16.26 and 17.45 nM for PI3Kδ and PI3Kγ, respectively.
LL-00084282 demonstrated high selectivity against PI3Kα and PI3Kβ with IC50 values of 582.1 nM and 342.0 nM, respectively.
LL-00084282 displayed no significant binding on human GPCRs, ion-channels and kinase panels from Eurofins Discovery.
In contrast to selective PI3Kδ inhibitors, LL-00084282 showed superior and potent anticancer activity in both ABC- and GCB-DLBCL cell lines.
LL-00084282 demonstrated in-vivo efficacy in OCI-Ly10 and SU-DHL-6 xenografts with good tolerability.
LL-00084282 inhibited pro-inflammatory cytokine secretion and reduced basophil activation in human PBMCs, showing potential implications in immunoinflammatory conditions.
