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Beschreibung

A cell-permeable pyrimido[1,2-a]pyrimidin-6(2H)-one derivative that acts as a potent, selective, and ATP competitive inhibitor of vacuolar protein sorting 34 kinase activity (Vps34, Kd = 1.5 nM, IC50 = 1.2 nM in a biochemical assay, and IC50 = 27 nM in a cell based assay). Does not affect the activity of over 200 other protein kinases including class I and II PI 3 kinases and mTOR (~ 10 microM). However, it displays a weak inhibitory activity against SMG1 at higher concentrations (IC50 = 1 microM). Does not affect the Akt phosphorylation even at higher concentrations (~10 microM), Shown to affect the late endosome-lysosome compartment formation and block the formation of autophagosomes in starved HeLa and H1299 cells (~ 1 microM). Acts synergistically with everolimus to block the proliferation of ACHN and 786-O renal tumor cells.