5-Pyrimidinecarboxamide, N-hydroxy-2-[[2-[[6-(6-methoxy-3-pyridinyl)-4-methyl-8-quinazolinyl]oxy]ethyl]methylamino]-

Uses

PI3K/HDAC-IN-2 is a potent dual PI3K/HDAC inhibitor with IC50s of 226 nM, 279 nM, 467 nM, 29 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively, and IC50s of 1.3 nM, 3.4 nM, 972 nM, 17 nM, 12 nM for HDAC1, HDAC2, HDC4, HDAC6, HDAC8, respectively. PI3K/HDAC-IN-2 exhibits PI3Kδ and class I and IIb HDAC selectivity. PI3K/HDAC-IN-2 has remarkable anticancer effects[1].

in vivo

IC 50

PI3Kα: 226 nM (IC₅₀); PI3Kβ: 279 nM (IC₅₀); PI3Kγ: 467 nM (IC₅₀); PI3Kδ: 29 nM (IC₅₀); HDAC1: 1.3 nM (IC₅₀); HDAC2: 3.4 nM (IC₅₀); HDAC4: 972 nM (IC₅₀); HDAC6: 17 nM (IC₅₀); HDAC8: 12 nM (IC₅₀)