PI3K-IN-2 (compound 10) is a potent and orally activePI3Kβ/δ(IC₅₀=7.1/8.6 nM) inhibitor with excellent selectivity versus PI3Kσ andPI3Kγ(IC₅₀=13/190 nM, respectively)^[1].

PI3K-IN-2 (compound 10) shows PI3Kβ cell IC₅₀1.1 nM in phosphatase and tensin homolog (PTEN) null MDA-MB-468 cell and PI3Kδ cellIC₅₀14 nM in Jeko-1 B-cell^[1].

PI3K-IN-2 shows profound pharmacodynamic modulation of AKT phosphorylation in PTEN-deficient PC3 prostate tumour bearing mice after oral administration and gave significant inhibition of tumour growth in the same xenograft model^[1].

525.54

C₂₈H₂₉F₂N₃O₅

1403458-28-5

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