.cp_wz table {border-top: твердое тело 1px #ccc; border-left: твердое тело 1px #ccc; } .cp_wz таблица td {border-right: 1px solid #ccc; нижняя граница: сплошной 1px #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 Молекулярный вес: \ n 335,36 ML167 - высокоселективный ингибитор Cdc2-подобной киназы 4 (Clk4) с IC50 136 нМ,> 10-кратная селективность для близкородственных киназ Clk1-3 и Dyrk1A /1B.
Биологическая активность
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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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Протокол (только для справки) Анализ киназы: [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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Конверсия различных модельных животных на основе BSA (значение на основе данных из проекта рекомендаций 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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Например, чтобы изменить дозу ресвератрола, используемую для мыши (22,4 мг / кг), на дозу, основанную на BSA для крысы, умножьте 22,4 мг / кг на коэффициент Km для мыши, а затем разделите на коэффициент Km для крыса. Этот расчет дает эквивалентную дозу ресвератрола для крыс 11,2 мг / кг.
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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 Химическая информация
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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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Калькулятор молярности Калькулятор разведения Калькулятор молекулярной массы
Группа Продуктов : Клеточный цикл > CDK ингибитор
