PI3K/HDAC-IN-2 is a potent dualPI3K/HDACinhibitor withIC₅₀s of 226 nM, 279 nM, 467 nM, 29 nM forPI3Kα,PI3Kβ,PI3Kγ,PI3Kδ, respectively, andIC₅₀s of 1.3 nM, 3.4 nM, 972 nM, 17 nM, 12 nM forHDAC1,HDAC2, HDC4,HDAC6,HDAC8, respectively. PI3K/HDAC-IN-2 exhibitsPI3Kδand class I and IIbHDACselectivity. PI3K/HDAC-IN-2 has remarkable anticancer effects^[1].

For PI3K/HDAC-IN-2 (Compound 8), the IC50 values in the growth inhibition assay against MDA-MB-453, HCT116 and HGC-27 cells are as low as namomolar level, which are 4 nM, 7 nM and 14 nM respectively^[1].
PI3K/HDAC-IN-2 (Compound 8) shows antiproliferative activities against 16 DLBCL cell lines with IC50s of 3.6-21 nM^[1].

In the zebrafish xenograft model of SU-DHL-4 cells, PI3K/HDAC-IN-2 (Compound 8) exhibits in vivo growth inhibitory activity at 3 μM^[1].

461.47

C₂₃H₂₃N₇O₄

2361418-65-5

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