DCLK1-IN-1
Based on 7 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).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.35%
- No. CAS: 2222635-15-4
- Fòrmula: C26H28F3N7O2
- Peso molecular:527.54
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) DCLK1-IN-1
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Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CAKI-1 | IC50 |
12.2 μM
Compound: DCLK1-IN-1
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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
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[PMID: 37862816] |
| HCT-116 | IC50 |
6.2 μM
Compound: DCLK1-IN-1
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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
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[PMID: 37862816] |
| HeLa | IC50 |
3350 nM
Compound: FMF-03-146-1; DCLK1-IN-1
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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
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[PMID: 32530623] |
| SW1990 | IC50 |
14 μM
Compound: DCLK1-IN-1
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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
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[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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2222635-15-4
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Appearance Solid
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Peso molecular 527.54
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Fòrmula C26H28F3N7O2
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Color Light yellow to yellow
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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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
2026 Jun;16(6):e70712. PMID: 42298903 -
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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 -
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (274 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
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.
| 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 |
DCLK1-IN-1 Related Classifications
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