CH-5132799 Mesylate

CH5132799 (PA-799) is a potent and orally active PI3Kα inhibitor (IC50=0.014 μM) with specific activity against class I PI3K and mutant isoforms. It demonstrates robust antiproliferative effects in vitro and induces significant tumor regression in vivo, particularly in models with PIK3CA mutations or activated PI3K pathway signaling.