Selective PI3Kδ Inhibitor 1

Biological Activity

Selective PI3Kδ Inhibitor 1 (compound 7n) is a PI3Kδ inhibitor with IC50 of 0.9 nM for PI3Kδ, which is more than 1000-fold selective for other class I PI3K isoforms. The IC50 values of it for PI3Kα/γ/β were 3670, 1460, and 21300 nM, respectively.

in vivo

Selective PI3Kδ Inhibitor 1 has favorable pharmacokinetic profile: good bioavailability and moderate in vivo half-life. In rats, its oral bioavailability was 41%; after intravenous injection, Vss, T _1/2 and CL were 2.8 L/kg, 3.4 h and 12 mL/min/kg, respectively .

target

Target	Value
PI3Kδ (Cell-free assay)	0.9 nM