DCLK1-IN-1

Catalog No.S8976 Batch:S897601

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Technical Data

Formula

C26H28F3N7O2
Molecular Weight 527.54 CAS No. 2222635-15-4
Solubility (25°C)* In vitro DMSO 95 mg/mL (180.08 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
1.18mg/ml Taking the 1 mL working solution as an example, add 50 μL of 23.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
1.18mg/ml Taking the 1 mL working solution as an example, add 50 μL of 23.6 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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]
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]

Protocol (from reference)

Cell Assay:

[1]
  • 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.
Animal Study:

[1]
  • Animal Models

    8–12-week-old male swiss albino mice

  • Dosages

    2 mg/kg, 10 mg/kg

  • Administration

    IV, Oral gavage

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

Targeting DCLK1 overcomes 5-fluorouracil resistance in colorectal cancer through inhibiting CCAR1/β-catenin pathway-mediated cancer stemness [ Clin Transl Med, 2022, 12(5):e743] PubMed: 35522902

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.