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DCLK1-IN-1

Name: DCLK1-IN-1
Brand: TargetMol
SKU: T8418
Price: 98 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T8418Cas No. 2222635-15-4

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.

DCLK1-IN-1

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Purity: 99.28%

Catalog No. T8418Cas No. 2222635-15-4

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$98	In Stock	In Stock
5 mg	$163	In Stock	In Stock
10 mg	$242	In Stock	In Stock
25 mg	$413	In Stock	In Stock
50 mg	$592	-	In Stock
100 mg	$848	-	In Stock
1 mL x 10 mM (in DMSO)	$189	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.28%

Appearance:Solid

Color:Yellow

Resource Download

COA LCMS HNMR

Product Introduction

DCLK1-IN-1 AI Summary

DCLK1-IN-1 is a bioactive molecule with diverse effects on various cellular and protein targets. It demonstrates potent inhibition of recombinant human N-terminal His6-tagged DCLK1 with an IC50 of 17.0 nM, and a moderate inhibitory effect on ERK5 in human HeLa cells with an IC50 of 3350.0 nM. It also shows a moderate inhibitory effect on recombinant human GST-tagged LRRK2 catalytic domain with an IC50 of 7000.0 nM, while exhibiting no significant inhibition of BRD4 bromodomain 1 in AlphaScreen displacement assays. In cytotoxicity assays, DCLK1-IN-1 reduces the viability of human Panc286 and Panc281 cell organoids by at least 50% at a concentration of 1 μM after 12 days. In HEK293T cells, its growth rate effect ranges from -0.03 to 0.36, in U2OS cells from 0.83 to 0.9, and in human fibroblast cells from -0.1 to 0.51, indicating varying effects on cell viability dependent on cell type. The compound also exhibits different effects on the protein stability of various domains in thermal shift assays, suggesting a complex pattern of interaction. Pharmacokinetic data in mouse studies show that DCLK1-IN-1 has a half-life of 2.09 hours, an AUC of 1269.5 ng·hr·mL⁻¹, and a clearance rate of 26.26 mL·min⁻¹·kg⁻¹..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	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.
In vitro	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]
In vivo	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]

Chemical Properties

Molecular Weight	527.54
Formula	C₂₆H₂₈F₃N₇O₂
Cas No.	2222635-15-4
Smiles	COc1cc(ccc1Nc1ncc2N(CC(F)(F)F)C(=O)c3ccccc3N(C)c2n1)N1CCN(C)CC1
Relative Density.	1.331 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 11.9 mg/mL (22.56 mM), Sonication is recommended.

In Vivo Formulation

2% DMSO+40% PEG300+5% Tween 80+53% Saline: 1 mg/mL (1.9 mM), Solution.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.8956 mL	9.4780 mL	18.9559 mL	94.7795 mL
5 mM	0.3791 mL	1.8956 mL	3.7912 mL	18.9559 mL
10 mM	0.1896 mL	0.9478 mL	1.8956 mL	9.4780 mL
20 mM	0.0948 mL	0.4739 mL	0.9478 mL	4.7390 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc