AZ191 1594092-37-1
Descripción del producto
.cp_wz tabla {borde superior: 1px sólido #ccc; borde izquierdo: 1px sólido #ccc; } .cp_wz table td {borde derecho: 1px sólido #ccc; borde inferior: 1px sólido #ccc; padding: 5px 0px 0px 5px;} .cp_wz table th {border-right: 1px solid #ccc; border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;} \ n Peso molecular: 429.52 AZ191 es un inhibidor de DYRK1B potente y selectivo con IC50 de 17 nM, una selectividad de aproximadamente 5 y 110 veces sobre DYRK1A y DYRK2, respectivamente. \ n Actividad biológica
Protocolo (solo como referencia) Ensayo de quinasa: [1]
Conversión de diferentes modelos de animales basados en BSA (valor basado en datos del Borrador de Directrices de la FDA)
Por ejemplo, para modificar la dosis de resveratrol utilizada para un ratón (22,4 mg / kg) a una dosis basada en el BSA para una rata, multiplique 22,4 mg / kg por el factor Km para un ratón y luego divida por el factor Km para una rata. Este cálculo da como resultado una dosis equivalente para ratas de resveratrol de 11,2 mg / kg.
Información química
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. | |||||
---|---|---|---|---|---|---|
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 |
|
|||||
Features |
|
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. |
---|
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 |
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 |
---|---|
Formula |
C24H27N7O |
CAS No. | 1594092-37-1 |
Storage | 3 years -20℃Powder |
---|---|
6 months-80℃in solvent (DMSO, water, etc.) | |
Synonyms | N/A |
Solubility (25°C) * | In vitro | DMSO | 86 mg/mL (200.22 mM) |
---|---|---|---|
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 |
---|
Otros productos
Productos hot
Astragalósido AClortetraciclina HCl 64-72-2Paclitaxel 33069-62-4Acetato de dexametasona 1177-87-3Dinaciclib (SCH727965) 779353-01-4CHIR-124 405168-58-3Ro3280 1062243-51-9TAME 901-47-3CCG-1423 285986-88-110058-F4 403811-55-2Dabigatrán (BIBR 953) 211914-51-1H 89 2HCl 130964-39-5T0901317 293754-55-9Aprepitant 170729-80-3Turofexorate Isopropil (XL335) 629664-81-9BMS-378806 357263-13-9