Home Metabolism Serine/threonin kinase inhibitor DCLK1-IN-1 For research use only.

DCLK1-IN-1

DCLK1-IN-1 is a selective, in vivo-compatible chemical probe of the doublecortin like kinase 1 (DCLK1) domain that binds to DCLK1 and DCLK2 with IC50 of 9.5 nM and 31 nM, respectively. DCLK1-IN-1 inhibits DCLK1 and DCLK2 kinases with IC50 of 57.2 nM and 103 nM in kinase assay, respectively.

DCLK1-IN-1 Chemical Structure

DCLK1-IN-1 Chemical Structure

CAS: 2222635-15-4

Selleck's DCLK1-IN-1 has been cited by 1 publication

Purity & Quality Control

Batch: S897601 DMSO] 95 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.71%
99.71

DCLK1-IN-1 Related Products

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Biological Activity

Description DCLK1-IN-1 is a selective, in vivo-compatible chemical probe of the doublecortin like kinase 1 (DCLK1) domain that binds to DCLK1 and DCLK2 with IC50 of 9.5 nM and 31 nM, respectively. DCLK1-IN-1 inhibits DCLK1 and DCLK2 kinases with IC50 of 57.2 nM and 103 nM in kinase assay, respectively.
Targets
DCLK1 [1]
(Cell-free assay)		 DCLK2 [1]
(Cell-free assay)		 DCLK1 [1]
(kinase assay)		 DCLK2 [1]
(kinase assay)
9.5 nM 31 nM 57.2 nM 103 nM
In vitro
In vitro

DCLK1-IN-1 displays pronounced on-target DCLK1 activity in vitro. DCLK1-IN-1 potently binds DCLK1 in HCT116 cells (IC50 = 279 nM). DCLK1-IN-1 significantly inhibits DCLK1, and weakly inhibits ERK5, in PATU-8988T cell lysates and live cells.[1]
Cell Research Cell lines PATU-8988T, PATU-8902, MIA PaCa-2, Panc03.27, CFPAC-1, BxPC-3, 293FT, HEK-293, HCT116 cells
Concentrations 1 μM, 2.5 μM
Incubation Time 4 h, 24 h
Method

For RNA-sequencing studies, PATU-8988T cells are plated at 200,000 cells per well in six-well plates. After adhering overnight, cells are treated with DMSO or 2.5 μM DCLK1-IN-1, washed twice with PBS, lysed and homogenized using Qiashredder columns.
In Vivo
In vivo

DCLK1-IN-1 has a favorable pharmacokinetic profile in mice, with a half-life of 2.09 h, an area under the curve of 5,506 h ng−1 ml−1 and 81% oral bioavailability. DCLK1-IN-1 is well-tolerated at doses up to 100 mg kg−1 with no adverse effects and no loss of body weight observed in mice. DCLK1-IN-1 is a selective inhibitor of DCLK1, suitable for use as a chemical probe when used together with control compound DCLK1-NEG.[1]
Animal Research Animal Models 8–12-week-old male swiss albino mice
Dosages 2 mg/kg, 10 mg/kg
Administration IV, Oral gavage

Chemical Information & Solubility

Molecular Weight 527.54 Formula

C26H28F3N7O2
CAS No. 2222635-15-4 SDF --
Smiles COC1=C(NC2=NC=C3N(CC(F)(F)F)C(=O)C4=CC=CC=C4N(C)C3=N2)C=CC(=C1)N5CCN(C)CC5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 95 mg/mL ( (180.08 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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