Formulation: A solid
Formal 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
Purity: ≥95%
Formula Markup: C26H28F3N7O2
Formula Weight: 527,5
Shelf life (days): 1460
CAS Number: 2222635-15-4
Notes: DCLK1-IN-1 is an inhibitor of doublecortin-like kinase 1 (DCLK1; IC50 = 17 nM).{69699} It is selective for DCLK1 over leucine-rich repeat kinase 2 (LRRK2), bromodomain-containing protein 4 (BRD4), and ERK5 (IC50s = 7,000, >10,000, and 3,350 nM, respectively). DCLK1-IN-1 (1 µM) reduces the number of cells in primary patient-derived pancreatic cancer organoids. In vivo, DCLK1-IN-1 (10 mg/kg every other day) reduces plaque area and collagen levels in the aortic arches and serum levels of Tnf-α and Il-6 an ApoE-/- mouse model of atherosclerosis induced by a high-fat diet.{69700}
English
Deutsch
