NSC 781406 is a dual inhibitor of PI3K and mammalian target of rapamycin (mTOR; IC50s = 2.0, 9.4, 2.7, 14, and 5.4 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, and mTOR, respectively). It inhibits cell growth in the NCI-60 panel of cancer cell lines (mean GI50 = 65 nM). NSC 781406 (30 mg/kg) reduces tumor volume in a BEL-7404 hepatic cancer mouse xenograft model.