| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
DYRK1A 220 nM (IC50) DYRK1A 3 nM (Kd) DYRK1B 56 nM (Kd)
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|---|---|
| ln Vitro |
DYRK1-IN-1 has an IC50 value of 220 nM, which inhibits DYRK1A's phosphorylation activity. With an IC50 value of 0.59 μM, DYRK1-IN-1 suppresses the phosphorylation of tau. Without P-glycoprotein liability, DYRK1-IN-1 has good permeability and cellular activity. strong physicochemical characteristics, high levels of enzymatic efficacy, strong aqueous solubility, outstanding kinome selectivity, and a promising inhibitory target in vitro are all displayed by DYRK1-IN-1. A 434 nM IC50 and an enzymatic IC50 of 75 nM demonstrate satisfactory cellular activity in DYRK1-IN-1 (HEK293 cells)[1].
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| ln Vivo |
The clearance of DYRK1-IN-1 (1 mg/kg; intravenous) is high[1].
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| Animal Protocol |
Animal/Disease Models: Sprague−Dawley rats[1]
Doses: 1 mg/kg (pharmacokinetic/PK Analysis) Route of Administration: Iv Experimental Results: High clearance was observed. |
| References |
[1]. Henderson SH, et al. Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors. J Med Chem. 2021;64(15):11709-11728.
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| Molecular Formula |
C12H12N6
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|---|---|
| Molecular Weight |
240.26
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| CAS # |
2814486-79-6
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Solubility (In Vitro) |
DMSO: 25 mg/mL (104.05 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1622 mL | 20.8108 mL | 41.6216 mL | |
| 5 mM | 0.8324 mL | 4.1622 mL | 8.3243 mL | |
| 10 mM | 0.4162 mL | 2.0811 mL | 4.1622 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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