Selective PI3Kδ Inhibitor 1 (compound 7n) is an inhibitor of PI3Kδ with an IC50 of 0.9 nM and >1000-fold selectivity against other class I PI3K isoforms [PI3K α/γ/β=3670/1460/21300 nM].
The compound shows reasonable pharmacokinetics with good bioavailability and moderate in vivo half-life. In rats, the oral bioavailability (F%) is 41, the Vss, T1/2 and CL are 2.8 L/kg, 3.4 h and 12 mL/min/kg respectively after IV administration[1].
[1] Terstiege I, et al. Bioorg Med Chem Lett. 2017, 27(3):679-687.