VPS34 Inhibitor, SAR405

Descrição detalhada : 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.
Sinónimos : VPS34 Inhibitor, SAR405; Vacuolar Protein Sorting 34 Inhibitor, SAR405, (S)-1-((5-chloropyridin-3-yl)methyl)-8-((R)-3-methylmorpholino)-2-(trifluoromethyl)-3,4-dihydro-1H-pyrimido[1,2-a]pyrimidin-6(2H)-one
Fórmula molecula r: C19H21ClF3N5O
Armazenamento : -20C
Embalagem : 1X1EA