Nemiralisib is a potent and highly selective inhibitor of PI3Kδ (pKi: 9.9).

Nemiralisib inhibits IFNγ in the peripheral blood mononuclear (PBMC) (pIC50: 9.7). Nemiralisib is highly selective for PI3Kδ. It has >1000-fold selectivity over the closely related isoforms PI3Kα (pIC50=5.3), PI3Kβ (pIC50=5.8), and PI3Kγ (pIC50=5.2)[1].

Nemiralisib free base is active in a disease-relevant brown norway rat acute OVA model of Type 2 helper T-cells (Th2)-driven lung inflammation. Pharmacokinetic data from Sprague Dawley male rats are obtained to assess the suitability of the series for inhaled delivery clearance data in rat microsomes and subsequently in vivo. Compounds (e.g., Nemiralisib) are administered by the oral or intravenous routes, at a dose level of 3 and 1mg/kg respectively (n=2 rats/route)[1].

1254036-71-9

C26H28N6O

440.54

GSK2269557 (free base);Nemiralisib

DMSO:31 mg/mL (70.37 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years