2222635-15-4

2222635-15-4 structure

Name: DCLK1-IN-1
Chemical Name: DCLK1-IN-1
CAS Number: 2222635-15-4
Molecular Formula: C₂₆H₂₈F₃N₇O₂
Molecular Weight: 527.54
Catalog: Signaling Pathways Others Others
Create Date: 2020-06-02 06:56:11
Modify Date: 2024-01-10 21:09:40
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].

Name	DCLK1-IN-1

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.