DCLK1-IN-1

2222635-15-4

527.54

DMSO : 35.71 mg/mL (67.69 mM; Need ultrasonic)

Others

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]. 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].