CHMFL-PI3KD-317 is a highly potent, selective, and orally active PI3Kδ inhibitor with an IC50 of 6 nM. It demonstrates over 10-1500 fold selectivity compared to other class I, II, and III PIKK family isoforms. The compound inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells with an EC50 of 4.3 nM and exhibits antiproliferative effects on cancer cells.
- Highly potent and selective PI3Kδ inhibitor
- Orally active
- Exhibits antiproliferative effects on cancer cells
- Favorable oral bioavailability
- Acceptable half-life