3006905-22-9

PI3K/HDAC-IN-3 (36) is a PI3K and HDAC dual inhibitor, with IC50 values of 0.23 nM and 172 nM for PI3Kα and HDAC1, respectively. PI3K/HDAC-IN-3 (36) suppresses AKT phosphorylation and increased H3 acetylation in MV4-11 cells. PI3K/HDAC-IN-3 (36) exhibits significant and dose-dependent anticancer efficacy in a MV4-11 xenograft model[1].

[1] Kehui Zhang, et al. Rational design and optimization of novel 4-methyl quinazoline derivatives as PI3K/HDAC dual inhibitors with benzamide as zinc binding moiety for the treatment of acute myeloid leukemia. Eur J Med Chem. 2023 Nov 30:264:116015. DOI:10.1016/j.ejmech.2023.116015