DM-PIT-1 inhibits in vivo tumor growth. (A) DM-PIT-1 encapsulation into PEG-PE micelles facilitates cytotoxicity of DM-PIT-1. U87MG cells were incubated with DM-PIT-1 or DM-PIT-1-M with or without 10 ng/mL TRAIL for 24 h, followed by cell viability analysis using ATP assay. (B) Administration of DM-PIT-1 or DM-PIT-1-M for 8 d attenuates syngeneic 4T1 beast tumor growth in BALB/c mice. After inoculation of tumor cells, DM-PIT-1 or DM-PIT-1-M was administered i.v. daily at doses of 0.4 and 1 mg/kg, respectively, for 8 d. The tumor volumes were measured every two days and are shown. (C) DM-PIT-1 and DM-PIT-1-M administration induces apoptosis of cancer cells in vivo measured with TUNEL assay (green), and nuclei were stained with Hoechst (blue). (D) DM-PIT-1 and DM-PIT-1-M administration suppresses PI3K/PIP3/Akt signaling, and increases cleavage of caspase-3 in tumor cells evaluated by using Western blot.