Description du produit
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Poids moléculaire :
335,36 ML167 est un inhibiteur hautement sélectif de la kinase 4 (Clk4) de type Cdc2 avec une IC50 de 136 nM, une sélectivité >10 fois pour les kinases étroitement apparentées Clk1-3 et Dyrk1A /1B.
Activité biologique
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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Protocole (uniquement pour référence) Dosage de la kinase : [1]
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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Conversion de différents animaux modèles sur la base de la BSA (valeur basée sur les données des lignes directrices provisoires de la FDA)
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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Par exemple, pour modifier la dose de resvératrol utilisée pour une souris (22,4 mg/kg) à une dose basée sur la BSA pour un rat, multiplier 22,4 mg/kg par le facteur Km pour une souris puis diviser par le facteur Km pour un rat. Ce calcul donne une dose équivalente chez le rat pour le resvératrol de 11,2 mg/kg.
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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Informations chimiques
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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Calculateur de molarité Calculateur de dilution Calculateur de poids moléculaire
Groupes de Produits : Cycle cellulaire > Inhibiteur CDK