A total of 24 anticancer agents including ZSTK474, other PI3K inhibitors, and those clinically used for sarcoma treatment were examined with respect to their antitumor profiles across the panel of sarcoma cell lines in terms of effects on tumor growth, PI3K-downstream signaling pathway alterations and apoptosis induction in vitro and in vivo. The gene discussed is PIK3CA; the disease is sarcoma.