| Zahlungsart: | T/T,L/C,Western Union |
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| Incoterm: | FOB |
| Minimum der Bestellmenge: | 1 Gram |
| Lieferzeit: | 8 Tage |
| Description | AZ191 is a potent and selective DYRK1B inhibitor with IC50 of 17 nM, about 5- and 110-fold selectivity over DYRK1A and DYRK2, respectively. | |||||
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| Targets | Dyrk1B [1] | DYRK1A [1] | DYRK2 [1] | |||
| IC50 | 17 nM | 88 nM | 1890 nM | |||
| In vitro | AZ191 selectively inhibits DYRK1B serine/threonine kinase activity with no effect on tyrosine kinase autophosphorylation. In HEK-293 cells, AZ191 also displays much greater potency for DYRK1B over DYRK1A, inhibiting CCND1 phosphorylation. In HD1B cells, AZ191 strongly inhibits the levels of the cell-cycle regulators, p21Cip1 and p27Kip1, and increases cell-cycle progression. | |||||
| In vivo |
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| Features |
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| In vitro DYRK kinase assay | EGFP–DYRK1A, EGFP–DYRK1B or EGFP–DYRK2 was immunoprecipitated from whole-cell lysate and pre-incubated in the absence or presence of various concentrations of AZ191 or harmine for 5 min at room temperature (20°C) and then assayed for kinase activity by incubating with 50 μM Woodtide, with two additional lysine residues attached to the N-terminus to allow it to bind to P81 paper (KKSSCYVDRKIYTYIQSRFY), 50 mM Tris/HCl (pH 7.5), 0.1 mM EGTA, 0.1% 2-mercaptoethanol, 10 mM MgCl2 and 0.1 mM [γ-32P]ATP in a total volume of 50 μl for 25 min at 30°C. |
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| Species | Baboon | Dog | Monkey | Rabbit | Guinea pig | Rat | Hamster | Mouse |
| Weight (kg) | 12 | 10 | 3 | 1.8 | 0.4 | 0.15 | 0.08 | 0.02 |
| Body Surface Area (m2) | 0.6 | 0.5 | 0.24 | 0.15 | 0.05 | 0.025 | 0.02 | 0.007 |
| Km factor | 20 | 20 | 12 | 12 | 8 | 6 | 5 | 3 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
Um die Dosis von Resveratrol für eine Maus (22,4 mg/kg) verwendet, um eine Dosis zu ändern z. B. basierend auf der BSA für eine Ratte, 22,4 mg/kg mit der K-m -Faktor für eine Maus multiplizieren und Dividieren Sie dann durch K-m -Faktor für eine Ratte. Diese Berechnung führt zu einer Ratte Äquivalentdosis für Resveratrol von 11,2 mg/kg
| Rat dose (mg/kg) = mouse dose (22.4 mg/kg) × | mouse Km(3) | = 11.2 mg/kg |
| rat Km(6) |
| Molecular Weight (MW) | 429.52 |
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| Formula |
C24H27N7O |
| CAS No. | 1594092-37-1 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in solvent (DMSO, water, etc.) | |
| Synonyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 86 mg/mL (200.22 mM) |
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| Water | <1 mg/mL ( | ||
| Ethanol | 1 mg/mL (2.32 mM) | ||
| Chemical Name | N-(2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)-4-(1-methyl-1H-pyrrolo[2,3-c]pyridin-3-yl)pyrimidin-2-amine |
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