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FD274 is a potent dual PI3K/mTOR inhibitor with inhibitory effects on PI3Kα/β/γ/δ and mTOR, with IC50s of 0.65 nM, 1.57 nM, 0.65 nM, 0.42 nM, and 2.03 nM, respectively. FD274 showed significant antiproliferative activity in AML cell line antiproliferative assays. FD274 exhibited dose-dependent pit tumor growth activity in an HL-60 xenograft model. FD274 has potential for use in acute myeloid leukemia studies.