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].
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].
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Ferguson FM, et al. Discovery of a selective inhibitor of doublecortin like kinase 1. Nat Chem Biol. 2020 Apr 6.
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