DCLK1-IN-1 is a selective, in vivo compatible chemical probe of the kinase domain of doublecortin-like kinase 1 (DCLK1) and a highly selective DCLK1/2 inhibitor with IC50 values ​​of 9.5/57.2 nM (DCLK1) and 31/103 nM (DCLK2) by binding and kinase assays, respectively. It has low toxicity and is used to study DCLK1 biology and determine its role in cancer.

METHODS: A NanoBRET tracer (TAE684-NanoBRET-590) was synthesized and a DCLK1 NanoBRET assay was developed to measure the effect of DCLK1-IN-1 on cell proliferation in HCT116 cells.
RESULTS The IC50 value of DCLK1-IN-1 against HCT116 cells was 279nM. [1]
METHODS: ACHN, 786-O, and CAKI-1 RCC cells were treated with DCLK1-IN-1 (0.5, 1, 5, 10 μM) and subjected to wound healing assays.
RESULTS DCLK1-IN-1 exerted a significant anti-migratory effect on ACHN, 786-O, and CAKI-1 RCC cells, with ACHN and CAKI-1 cells showing a typical dose-dependent decrease in wound healing from 0.5 to 10 μM, while 786-O cells showed a significant decrease at a dose of 10 μM. [2]

DCLK1-IN-1 (3 mg/kg, intravenous injection; 10 mg/kg, oral administration) has good pharmacokinetic characteristics in mice, with a half-life of 2.09 hours, an area under the curve (AUCinf) of 5506 hr*ng/mL, and an oral bioavailability of 81%. [1]