PI-103 is a potent, dual class I PI3K/mTOR inhibitor with IC50 of 2/3/3/15/ for p110α/β/δ/γ, respectively.
PI-103 also inhibits TORC1 (>80% inhibition at 0.5 uM) and DNA-PK (IC50=14 nM), 15- to 20-fold less activity against class II PI3K C2β (IC50=43 nM), >1,300-fold selectivity over the class III PI3K Vsp34.
PI-103 potently inhibits proliferation and invasion of a wide variety of human cancer cells in vitro.
PI-103 shows activity in cancer xenograft models.
