Dyrk1A-IN-4
Based on 1 Customer Validation
Dyrk1A-IN-4 is a potent and orally active Dyrk1A inhibitor. Dyrk1A-IN-4 exhibits IC50s against DYRK1A and DYRK2 of 2 nM and 6 nM. Dyrk1A-IN-4 exhibits the inhibition of the DYRK1A pSer520 autophosphorylation in U2OS cells with an IC50 of 28 nM. Dyrk1A-IN-4 can be used for the studies of ovarian adenocarcinoma, neuroblastoma and cervical squamous cell carcinoma.
For research use only. We do not sell to patients.
- Purity: 99.30%
- CAS No.: 2091883-59-7
- Formula: C14H13F3N6
- Molecular Weight:322.29
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
DYRK1A 2 nM (IC50) |
DYRK2 6 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
1099 nM
Compound: 48
|
Antiproliferative activity against human A2780 cells assessed as reduction in cell viability incubated for 120 hrs by MTT assay
Antiproliferative activity against human A2780 cells assessed as reduction in cell viability incubated for 120 hrs by MTT assay
|
[PMID: 33975430] |
| A2780 | IC50 |
13 nM
Compound: 48
|
Antiproliferative activity against human A2780 cells assessed as reduction in cell viability by soft agar assay
Antiproliferative activity against human A2780 cells assessed as reduction in cell viability by soft agar assay
|
[PMID: 33975430] |
| C-33-A | IC50 |
1154 nM
Compound: 48
|
Antiproliferative activity against human C-33-A cells assessed as reduction in cell viability incubated for 120 hrs by MTT assay
Antiproliferative activity against human C-33-A cells assessed as reduction in cell viability incubated for 120 hrs by MTT assay
|
[PMID: 33975430] |
| C-33-A | IC50 |
21 nM
Compound: 48
|
Antiproliferative activity against human C-33-A cells assessed as reduction in cell viability by soft agar assay
Antiproliferative activity against human C-33-A cells assessed as reduction in cell viability by soft agar assay
|
[PMID: 33975430] |
| HT-22 | IC50 |
7.7 μM
Compound: 26
|
Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
|
[PMID: 36876904] |
| SK-N-MC | IC50 |
1281 nM
Compound: 48
|
Antiproliferative activity against human SK-N-MC cells assessed as reduction in cell viability incubated for 120 hrs by MTT assay
Antiproliferative activity against human SK-N-MC cells assessed as reduction in cell viability incubated for 120 hrs by MTT assay
|
[PMID: 33975430] |
| SK-N-MC | IC50 |
31 nM
Compound: 48
|
Antiproliferative activity against human SK-N-MC cells assessed as reduction in cell viability by soft agar assay
Antiproliferative activity against human SK-N-MC cells assessed as reduction in cell viability by soft agar assay
|
[PMID: 33975430] |
Dyrk1A-IN-4 (Compound 48) has an IC50 value of 13, 31 and 21 nM against A2780 cells, SK-N-MC cells and C-33A cells in a 3D tumor sphere model. [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:RS4;11 induced xenografted tumor model established in BALB/c nude female mice[1]
-
Dosage:6.25 mg/kg
-
Administration:Oral administration (p.o.), single dose
-
Result:Demonstrated a very strong and sustained inhibition of pDYRK1A (93% after 2 h and 95% after 6 h).
Chemical Information
-
CAS No. 2091883-59-7
-
Appearance Solid
-
Molecular Weight 322.29
-
Formula C14H13F3N6
-
Color Off-white to light yellow
-
SMILES
FC(F)(CN1C2=C(N=C1C)C=CC(C3=CC(N)=NC(N)=C3)=N2)F
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (310.28 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: 2.5 mg/mL (7.76 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (7.76 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal 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
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.
Purity & Documentation
-
Data Sheet (272 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
References
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1028 mL | 15.5140 mL | 31.0280 mL | 77.5699 mL |
| 5 mM | 0.6206 mL | 3.1028 mL | 6.2056 mL | 15.5140 mL | |
| 10 mM | 0.3103 mL | 1.5514 mL | 3.1028 mL | 7.7570 mL | |
| 15 mM | 0.2069 mL | 1.0343 mL | 2.0685 mL | 5.1713 mL | |
| 20 mM | 0.1551 mL | 0.7757 mL | 1.5514 mL | 3.8785 mL | |
| 25 mM | 0.1241 mL | 0.6206 mL | 1.2411 mL | 3.1028 mL | |
| 30 mM | 0.1034 mL | 0.5171 mL | 1.0343 mL | 2.5857 mL | |
| 40 mM | 0.0776 mL | 0.3878 mL | 0.7757 mL | 1.9392 mL | |
| 50 mM | 0.0621 mL | 0.3103 mL | 0.6206 mL | 1.5514 mL | |
| 60 mM | 0.0517 mL | 0.2586 mL | 0.5171 mL | 1.2928 mL | |
| 80 mM | 0.0388 mL | 0.1939 mL | 0.3878 mL | 0.9696 mL | |
| 100 mM | 0.0310 mL | 0.1551 mL | 0.3103 mL | 0.7757 mL |
Powered by Bioz