PI3Kα-IN-12 (compound 13) is a highly selective PI3Kα inhibitor ( IC 50 : 1.2 nM). PI3Kα-IN-12 inhibits HCT-116 and U87-MG with IC 50 s values of 0.83 and 1.25 μM, respectively. PI3Kα-IN-12 (40 mg/kg; IP ) causes tumor regression in a U87-MG cell line xenograft mouse model.
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