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DCLK1-IN-1

Names

[ CAS No. ]:
2222635-15-4

[ Name ]:
DCLK1-IN-1

Biological Activity

[Description]:

DCLK1-IN-1 is a selective, oral bioavailability in vivo-compatible chemical probe of the doublecortin like kinase 1 (DCLK1 kinase) domain. DCLK1-IN-1 inhibits DCLK1 and DCLK2 kinases (IC50: DCLK1=9.5/57.2 nM and DCLK2=31/103 nM in binding and kinase assay, respectively). DCLK1-IN-1 shows low toxicity, and can investigate DCLK1 biology and establish its role in cancer, like DCLK1+ pancreatic ductal adenocarcinoma (PDAC)[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Others >> Others

[In Vitro]

DCLK1-IN-1 shows no significant activity against ERK5, ACK, and LRRK2. DCLK1-IN-1 potently binds DCLK1 in HCT116 cells (IC50 = 279 nM). DCLK1-IN-1 significantly inhibited DCLK1, and weakly inhibited ERK5, in PATU-8988T cell lysates and live cells[1].

[In Vivo]

DCLK1-IN-1 has a favorable pharmacokinetic profile in mice, with a half-life of 2.09 hours, an area under the curve of 5,506 h/ng ml and 81% oral bioavailability[1].

[References]

[1]. Ferguson FM, et al. Discovery of a selective inhibitor of doublecortin like kinase 1. Nat Chem Biol. 2020 Apr 6.

Chemical & Physical Properties

[ Molecular Formula ]:
C26H28F3N7O2

[ Molecular Weight ]:
527.54

[ Storage condition ]:
-20°C

Related Compounds