2. Protein Tyrosine Kinase/RTK
  3. DYRK
  4. Dyrk1A-IN-4

Dyrk1A-IN-4 (compound 48) is a potent and orally active DYRK1A and DYRK2 inhibitor with IC50s of 2 nM and 6 nM, respectively. Dyrk1A-IN-4 has anticancer effects.

For research use only. We do not sell to patients.

Dyrk1A-IN-4 Chemical Structure

Dyrk1A-IN-4 Chemical Structure

CAS No. : 2091883-59-7

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5 mg USD 590 In-stock
10 mg USD 950 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Dyrk1A-IN-4 Related Antibodies

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DYRK1 DYRK2 DYRK4

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  • Purity & Documentation

  • References

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Description

Dyrk1A-IN-4 (compound 48) is a potent and orally active DYRK1A and DYRK2 inhibitor with IC50s of 2 nM and 6 nM, respectively. Dyrk1A-IN-4 has anticancer effects[1].

IC50 & Target[1]

DYRK1A

2 nM (IC50)

DYRK2

6 nM (IC50)

Molecular Weight

322.29

Formula

C14H13F3N6
CAS No.
Appearance

Solid

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
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1028 mL 15.5140 mL 31.0280 mL
5 mM 0.6206 mL 3.1028 mL 6.2056 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.90%

COA (247 KB) HNMR (154 KB) LCMS (374 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
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Dyrk1A-IN-4 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Dyrk1A-IN-42091883-59-7DYRKDual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinaseDYRK1ADYRK2orally activeanticancerInhibitorinhibitorinhibit

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