Chemical Name: 5,11-Dihydro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-11-methyl-5-(2,2,2-trifluoroethyl)-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one
Biological ActivityPotent and selective doublecortin like kinase 1/2 (DCLK1/2) inhibitor (IC50 values are DCLK1 =9.5 and 57.2 nM and DCLK2 = 31 and 103 nM in binding and kinase assay, respectively). Exhibits no significant activity against ERK5, ACK, BRD4 and LRRK2. Exhibits DCLK inhibition in pancreatic ductal adenocarcinoma (PDAC) organoid models. Orally bioavailable.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Discovery of a selective inhibitor of doublecortin like kinase 1.
Ferguson et al.
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