Chemical Name: N-[2-Chloro-5-[[[(3-chlorophenyl)methyl]amino]carbonyl]phenyl]-7,8-dihydro-2-methoxy-7-oxopyrido[2,3-d]pyrimidine-6-carboxamide
Biological ActivityPotent and selective DYRK1A/B inhibitor (IC50 values are 22 and 68 nM respectively). Selective for DYRK1A/B over a panel of other kinases. Reduces accumulation of quiescent Panc1 pancreatic cancer cells in G0 under serum free conditions. Also induces DNA damage and apoptosis in quiescent Panc1 cells.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Inactivation of mirk/dyrk1b kinase targets quiescent pancreatic cancer cells.
Ewton et al.
Mol.Cancer Ther., 2011;10:2104
Pyrido[2,3-d]pyrimidines: discovery and preliminary SAR of a novel series of DYRK1B and DYRK1A inhibitors.
Anderson et al.
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