The phosphatidylinositol 3-kinase (PI3K) signaling pathway has central roles in cell growth, development, and survival. GDC-0941 is a potent pan inhibitor of class I catalytic subunits of PI3K, inhibiting p110α, β, δ, and γ with IC50 values of 3, 33, 3, and 75 nM, respectively. It is much less effective against class II-IV isoforms of PI3K and against mTOR. GDC-0941 inhibits the growth of certain types of cancer cells and blocks signaling through PI3K to Akt, both in cells and in vivo.