Art. -Nr.: HY-135985

DCLK1-IN-1

6 Cited Publications

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Based on 6 publication(s) in Google Scholar

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).

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Reinheit: 99.35%
CAS. Nr.: 2222635-15-4
Formel: C₂₆H₂₈F₃N₇O₂
Molecular Weight:527.54

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

DCLK1-IN-1 Chemical Structure

CAS. Nr.: 2222635-15-4

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (6)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
CAKI-1	IC₅₀	12.2 μM Compound: DCLK1-IN-1	Antiproliferative activity against human CAKI-1 cells assessed as inhibition cell proliferation incubated for 6 days by MTT assay Antiproliferative activity against human CAKI-1 cells assessed as inhibition cell proliferation incubated for 6 days by MTT assay	[PMID: 37862816]
HCT-116	IC₅₀	6.2 μM Compound: DCLK1-IN-1	Antiproliferative activity against human HCT-116 cells assessed as inhibition cell proliferation incubated for 6 days by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition cell proliferation incubated for 6 days by MTT assay	[PMID: 37862816]
HeLa	IC₅₀	3350 nM Compound: FMF-03-146-1; DCLK1-IN-1	Inhibition of ERK5 in human HeLa cells assessed as reduction in EGF-induced ERK5 autophosphorylation pretreated for 1 hr followed by EGF stimulation and measured after 17 mins by 32p kinase assay Inhibition of ERK5 in human HeLa cells assessed as reduction in EGF-induced ERK5 autophosphorylation pretreated for 1 hr followed by EGF stimulation and measured after 17 mins by 32p kinase assay	[PMID: 32530623]
SW1990	IC₅₀	14 μM Compound: DCLK1-IN-1	Antiproliferative activity against human SW1990 cells assessed as inhibition cell proliferation incubated for 6 days by MTT assay Antiproliferative activity against human SW1990 cells assessed as inhibition cell proliferation incubated for 6 days by MTT assay	[PMID: 37862816]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 5506 h/ng mL and 81% oral bioavailability^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 2222635-15-4
Appearance Solid
Molecular Weight 527.54
Formel C₂₆H₂₈F₃N₇O₂
Color Light yellow to yellow
SMILES

O=C1N(CC(F)(F)F)C2=CN=C(NC3=CC=C(N4CCN(C)CC4)C=C3OC)N=C2N(C)C5=CC=CC=C15
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (6)

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Journal Impact Factor

Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Nat Commun

Targeting leucine-rich repeat kinase 2 overcomes resistance to oncolytic herpes simplex virus-based therapies in glioblastoma. [Abstract]

2026 Feb 28;17(1):3324. PMID: 41764166
J Biomed Sci

Doublecortin-like kinase 1 promotes fibroblast activation and fibrotic progression through Smad3 binding in idiopathic pulmonary fibrosis. [Abstract]

2026 May 22;33(1):52. PMID: 42174588
Clin Transl Med

DCLK1-dependent NF-κB activation mediates p-STAT3-induced osteoarthritis progression. [Abstract]

2026 Jun;16(6):e70712. PMID: 42298903
Cancers (Basel)

Inhibition of DCLK1 with DCLK1-IN-1 Suppresses Renal Cell Carcinoma Invasion and Stemness and Promotes Cytotoxic T-Cell-Mediated Anti-Tumor Immunity. [Abstract]

2021 Nov 16;13(22):5729. PMID: 34830884
bioRxiv

2025 Nov 7.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 35.71 mg/mL (67.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8956 mL

9.4780 mL

18.9559 mL

5 mM

0.3791 mL

1.8956 mL

3.7912 mL

10 mM

0.1896 mL

0.9478 mL

1.8956 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (3.94 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.94 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Ferguson FM, et al. Discovery of a selective inhibitor of doublecortin like kinase 1. Nat Chem Biol. 2020 Apr 6. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8956 mL	9.4780 mL	18.9559 mL	47.3898 mL
	5 mM	0.3791 mL	1.8956 mL	3.7912 mL	9.4780 mL
	10 mM	0.1896 mL	0.9478 mL	1.8956 mL	4.7390 mL
	15 mM	0.1264 mL	0.6319 mL	1.2637 mL	3.1593 mL
	20 mM	0.0948 mL	0.4739 mL	0.9478 mL	2.3695 mL
	25 mM	0.0758 mL	0.3791 mL	0.7582 mL	1.8956 mL
	30 mM	0.0632 mL	0.3159 mL	0.6319 mL	1.5797 mL
	40 mM	0.0474 mL	0.2369 mL	0.4739 mL	1.1847 mL
	50 mM	0.0379 mL	0.1896 mL	0.3791 mL	0.9478 mL
	60 mM	0.0316 mL	0.1580 mL	0.3159 mL	0.7898 mL

Keywords

DCLK1-IN-1

6 Cited Publications

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DCLK1-IN-1

Publications Citing Use of MedChemExpress (MCE) DCLK1-IN-1

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

DCLK1-IN-1 Related Classifications

HY-135985 Related Classifications