| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
AZ191 is a potent and selective DYRK1B (Dual-specificity tyrosine phosphorylation-regulated kinase) inhibitor with IC50 of 17 nM in a cell-free assay, about 5- and 110-fold selectivity over DYRK1A and DYRK2, respectively. Tyrosine kinase autophosphorylation is unaffected by AZ191, which specifically inhibits DYRK1B serine/threonine kinase activity. Moreover, AZ191 inhibits CCND1 phosphorylation in HEK-293 cells with significantly more potency against DYRK1B than DYRK1A. AZ191 accelerates cell-cycle progression in HD1B cells by potently suppressing the levels of the cell-cycle regulators, p21Cip1 and p27Kip1.
| Targets |
DYRK1B (IC50 = 17 nM); DYRK1A (IC50 = 88 nM)
|
||
|---|---|---|---|
| ln Vitro |
|
||
| ln Vivo |
|
||
| Cell Assay |
AZ191 at 1uM was unable to selectively inhibit DYRK1B serine/threonine kinase activity or inhibit DYRK1B autophospho-Tyr273 in HEK-293 cells. At doses as low as 30–100 nM, AZ191 inhibited phosphorylation of CCND1 with greater potency for DYRK1B over DYRK1A in HEK-293 cells co-expressing CCND1 with either DYRK1A or DYRK1B. With approximately 100-fold selectivity over DYRK2 and 5–10-fold selectivity over DYRK1A, AZ191 is a novel inhibitor that selectively targets DYRK1B. To identify DYRK1B substrates and functions, AZ191 will be a helpful probe.
|
||
| Animal Protocol |
|
||
| References |
|
| Molecular Formula |
C24H27N7O
|
|
|---|---|---|
| Molecular Weight |
429.52
|
|
| Exact Mass |
429.23
|
|
| Elemental Analysis |
C, 67.11; H, 6.34; N, 22.83; O, 3.72
|
|
| CAS # |
1594092-37-1
|
|
| Related CAS # |
|
|
| Appearance |
Brown solid powder
|
|
| SMILES |
CN1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=CC(=N3)C4=CN(C5=C4C=CN=C5)C)OC
|
|
| InChi Key |
ZYVXTMKTGDARKR-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C24H27N7O/c1-29-10-12-31(13-11-29)17-4-5-21(23(14-17)32-3)28-24-26-9-7-20(27-24)19-16-30(2)22-15-25-8-6-18(19)22/h4-9,14-16H,10-13H2,1-3H3,(H,26,27,28)
|
|
| Chemical Name |
N-[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]-4-(1-methylpyrrolo[2,3-c]pyridin-3-yl)pyrimidin-2-amine
|
|
| Synonyms |
|
|
| HS Tariff Code |
2934.99.9001
|
|
| 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)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.82 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 25.0 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: 2.5 mg/mL (5.82 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3282 mL | 11.6409 mL | 23.2818 mL | |
| 5 mM | 0.4656 mL | 2.3282 mL | 4.6564 mL | |
| 10 mM | 0.2328 mL | 1.1641 mL | 2.3282 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.
|
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
