PI3K-α Inhibitor

PI3Kα inhibitor is a potent and selective inhibitor of PI3Kα with IC₅₀ values of 2, 16, 660, and 220 nM for the α, β, γ, and 2Cβ isoforms, respectively. It inhibits PKA, KDR, PKCα, and cyclin E/Cdk2 significantly less effectively (IC₅₀ = 91, 3.4, 466, and 28 µM, respectively). PI3Kα inhibitor inhibits A375 melanoma cell proliferation with an IC₅₀ value of 580 nM.