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DCLK1-IN-1 Serine/threonin kinase inhibitor

Name: DCLK1-IN-1
Brand: Selleck Chemicals
SKU: S8976
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S8976

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. This compound inhibits DCLK1 and DCLK2 kinases with IC50 of 57.2 nM and 103 nM in kinase assay, respectively.

Chemical Structure

Molecular Weight: 527.54

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.71

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Other Serine/threonin kinase Products	WNK463 SRPIN340 Benzamidine HCl SPHINX31 GCN2iB WNK-IN-11 14-3-3 η Antibody [G4H24] MKI-1 STK16-IN-1 2OH-BNPP1

Solubility

In vitro
Batch:

DMSO : 95 mg/mL (180.08 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.180mg/ml (2.24mM)	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.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.180mg/ml (2.24mM)	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.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	527.54	Formula	C₂₆H₂₈F₃N₇O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2222635-15-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			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

Mechanism of Action

Targets/IC₅₀/Ki	DCLK1 (Cell-free assay) 9.5 nM DCLK2 (Cell-free assay) 31 nM DCLK1 (kinase assay) 57.2 nM DCLK2 (kinase assay) 103 nM
In vitro	DCLK1-IN-1 displays pronounced on-target DCLK1 activity in vitro. This compound potently binds DCLK1 in HCT116 cells (IC50 = 279 nM). It significantly inhibits DCLK1, and weakly inhibits ERK5, in PATU-8988T cell lysates and live cells.
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. This compound is well-tolerated at doses up to 100 mg kg⁻¹ with no adverse effects and no loss of body weight observed in mice. It is a selective inhibitor of DCLK1, suitable for use as a chemical probe when used together with control compound DCLK1-NEG.
References	[1] https://pubmed.ncbi.nlm.nih.gov/32251410/

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