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| 10mg |
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| Targets |
AZ-Dyrk1B-33 targets Dyrk1B (dual-specificity tyrosine-phosphorylation-regulated kinase 1B), a kinase involved in various cellular processes including cell cycle regulation and survival. By competitively binding to the ATP-binding site of Dyrk1B, it inhibits its kinase activity. The compound demonstrates cellular in vitro activity with an IC50 of 194 nM.
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| ln Vitro |
AZ-Dyrk1B-33 has an IC50 of 0.192 μM and can prevent Dyrk pS421 from being phosphorylated in cells[1]. There is no sensitization in AZ-Dyrk1B-33 [1].
In vitro, AZ-Dyrk1B-33 has demonstrated cellular activity with an IC50 of 194 nM. It is a potent inhibitor of Dyrk1B kinase activity in cell-free assays. The compound shows no off-target effects against a panel of 124 kinases tested, with no kinase inhibited above 50% at 1 µM. |
| ln Vivo |
Specific in vivo data for AZ-Dyrk1B-33 are not detailed in the available literature. However, as a potent and selective kinase inhibitor, it is expected to be used in preclinical studies to investigate the role of Dyrk1B in various disease models, including cancer. Its selectivity profile suggests it could be a valuable tool for in vivo target validation.
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| Enzyme Assay |
The enzymatic activity of AZ-Dyrk1B-33 is assessed using kinase assays with recombinant Dyrk1B protein. The assay involves incubating the kinase with a peptide substrate and ATP in the presence of varying concentrations of the inhibitor. The extent of phosphorylation is measured using techniques such as radioactive labeling (e.g., 33P-ATP) or fluorescence-based detection. The IC50 value of 7 nM is determined from dose-response curves.
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| Cell Assay |
To evaluate the cellular effects of AZ-Dyrk1B-33, cells are treated with the compound at various concentrations, and the phosphorylation of Dyrk1B substrates is measured by Western blotting. Cell viability and proliferation are assessed using standard assays. The cellular IC50 of 194 nM is determined from dose-response curves. The distinct cellular effects compared to siRNA knockdown suggest the compound may have unique properties.
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| Animal Protocol |
In vivo studies with AZ-Dyrk1B-33 would typically involve administration to tumor-bearing mice in xenograft models. The compound would be given via oral or intraperitoneal routes at various doses. Tumor growth inhibition, body weight, and overall health are monitored to assess efficacy and tolerability. Pharmacodynamic markers, such as Dyrk1B phosphorylation levels in tumor tissue, would be measured.
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| ADME/Pharmacokinetics |
AZ-Dyrk1B-33 has a molecular formula of C19H16N4 and a molecular weight of 300.36. It is soluble in DMSO and 1 equivalent HCl. The compound should be stored at +4°C. It has a purity of ≥98% (HPLC).
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| Toxicity/Toxicokinetics |
Specific toxicology data for AZ-Dyrk1B-33 are not detailed in the available literature. However, its high selectivity for Dyrk1B over a panel of 124 kinases suggests a potentially lower risk of off-target toxicity. As with all research compounds, standard safety precautions should be taken during handling.
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| References | |
| Additional Infomation |
AZ-Dyrk1B-33 is a research tool for studying the biological role of Dyrk1B kinase. It has been used to explore a MEK resistance hypothesis. The compound's selectivity and potency make it a valuable chemical probe for investigating Dyrk1B function in various cellular processes and disease contexts, including cancer. It is not a clinically approved drug.
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| Molecular Formula |
C19H16N4
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|---|---|
| Molecular Weight |
300.3571434021
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| Exact Mass |
300.137
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| CAS # |
1679330-37-0
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| PubChem CID |
118735338
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
2.9
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
382
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1(C=C(C2C=CN=C(C)N=2)C2C=CN=CC1=2)CC1C=CC=CC=1
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| InChi Key |
CZCUSHJQJWKYTD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H16N4/c1-14-21-10-8-18(22-14)17-13-23(12-15-5-3-2-4-6-15)19-11-20-9-7-16(17)19/h2-11,13H,12H2,1H3
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| Chemical Name |
1-benzyl-3-(2-methylpyrimidin-4-yl)pyrrolo[2,3-c]pyridine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~416.17 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.93 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.93 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3293 mL | 16.6467 mL | 33.2934 mL | |
| 5 mM | 0.6659 mL | 3.3293 mL | 6.6587 mL | |
| 10 mM | 0.3329 mL | 1.6647 mL | 3.3293 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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