.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; relleno: 5px 0px 0px 5px;} \ n Peso molecular: \ n 335,36 ML167 es un inhibidor de quinasa 4 (Clk4) similar a Cdc2 altamente selectivo con IC50 de 136 nM, selectividad> 10 veces para quinasas estrechamente relacionadas Clk1-3 y Dyrk1A /1B.
Actividad biológica
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Description
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ML167 is a highly selective Cdc2-like kinase 4 (Clk4) inhibitor with IC50 of 136 nM, >10-fold selectivity for closely related kinases Clk1-3 and Dyrk1A/1B.
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Targets
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CLK4 [1]
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CLK1 [1]
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CLK2 [1]
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Dyrk1B [1]
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IC50
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136 nM
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1522 nM
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1648 nM
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4420 nM
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In vitro
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ML167, as a probe of Clk4, shows high cell permeability in a Caco-2 assay.
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In vivo
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Features
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Protocolo (solo como referencia) Ensayo de quinasa: [1]
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Bioluminescent assay
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Two bioluminescent assays are used for the Clk4 assay. Measurement of ATP depletion is assessed by using the Kinase-Glo™ assay system, where a firefly luciferase detection reagent containing D-luciferin and buffer components are added to detect the remaining ATP, following the Clk4 kinase assay. The second system, ADP-Glo® measures kinase activity by quantifying the amount of ADP formed after the kinase reaction. Bioluminescent detection of ADP levels is achieved through the addition two different detection reagents. First, a reagent that stops the protein kinase reaction and depletes the remaining ATP is added. Then, a second reagent is added to stop ATP degradation. In addition, the second reagent also contains an enzyme, such as pyruvate kinase, that efficiently converts the ADP to ATP and the same firefly luciferase/D-luciferin components present in Kinase-Glo, which generate the luminescent signal proportional to the ADP concentration produced. Therefore, the two assay formats show opposite luminescent signal changes in response to protein kinase inhibitors.
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Conversión de diferentes modelos de animales basados en BSA (valor basado en datos del Borrador de Directrices de la FDA)
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Species
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Baboon
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Dog
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Monkey
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Rabbit
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Guinea pig
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Rat
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Hamster
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Mouse
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Weight (kg)
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12
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10
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3
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1.8
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0.4
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0.15
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0.08
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0.02
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Body Surface Area (m2)
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0.6
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0.5
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0.24
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0.15
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0.05
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0.025
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0.02
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0.007
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Km factor
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20
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20
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12
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12
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8
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6
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5
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3
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Animal A (mg/kg) = Animal B (mg/kg) multiplied by
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Animal B Km
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Animal A Km
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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.
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Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×
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mouse Km(3)
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= 11.2 mg/kg
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rat Km(6)
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\ n Información química
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Molecular Weight (MW)
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335.36
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Formula
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C19H17N3O3
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CAS No.
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1285702-20-6
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Storage
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3 years -20℃Powder
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6 months-80℃in solvent (DMSO, water, etc.)
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Synonyms
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CID 44968231
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Solubility (25°C) *
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In vitro
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DMSO
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67 mg/mL
(199.78 mM)
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Water
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<1 mg/mL
(
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Ethanol
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13 mg/mL
heating
(38.76 mM)
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* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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Chemical Name
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5-[4-[[(5-Methyl-2-furanyl)methyl]amino]-6-quinazolinyl]-2-furanmethanol
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Calculadora de molaridad Calculadora de dilución Calculadora de peso molecular
Grupos de Producto : Ciclo celular > Inhibidor de CDK
