LDC000067 1073485-20-7
Описание продукта
.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 370,43 LDC000067 - высокоселективный ингибитор CDK9 с IC50 44 нМ, 55/125/210 /> 227 /> 227-кратная селективность по сравнению с CDK2 / 1/4 / 6/7. \ n Биологическая активность
Протокол (только для справки) Анализ киназы: [1]
Конверсия различных модельных животных на основе BSA (значение на основе данных из проекта рекомендаций FDA)
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.
Химическая информация
Калькулятор молярности Калькулятор разведения Калькулятор молекулярной массы
Description | LDC000067 is a highly selective CDK9 inhibitor with IC50 of 44 nM, 55/125/210/ >227/ >227-fold selectivity over CDK2/1/4/6/7. | |||||
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Targets | CDK9 [1] | CDK2 [1] | CDK1 [1] | CDK4 [1] | CDK6 [1] | CDK7 [1] |
IC50 | 44 nM | 2.441 μM | 5.513 μM | 9.242 μM | >10 μM | >10 μM |
In vitro | LDC000067 reduces Ser2-P, induces p53 activation and leads to apoptosis in mESCs. In addition, LDC067 also dose-dependently inhibits P-TEFb-dependent de novo RNA synthesis of cellular genes. | |||||
In vivo |
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Features | CDK9-selective inhibitor. |
In vitro enzymic kinase assay for CDKs | The FRET-based LANCE Ultra KinaSelect Ser/Thr kit is used to determine IC50 values for various CDK inhibitors. Kinase activity and inhibition in this assay is measured as recommended by the manufacturer. Briefly, a specific ULight MBP peptide substrate (50 nM final concentration) is phosphorylated by a CDK-cyclin pair in buffer (50 mM HEPES-KOH pH 7.5, 10 mM MgCl2, 1 mM EGTA, 2 mM dithiothreitol) containing ATP at the concentration of the KM values of the individual kinases for 1 h at room temperature. Subsequently, phosphorylation is detected by addition of specific Eu-labelled anti-phospho-antibodies (2 nM), which upon binding to the phosphopeptide give rise to a FRET signal. FRET signals are recorded in a time-resolved manner in a Perkin Elmer EnVision reader. |
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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 |
Rat dose (mg/kg) = mouse dose (22.4 mg/kg) × | mouse Km(3) | = 11.2 mg/kg |
rat Km(6) |
Molecular Weight (MW) | 370.43 |
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Formula |
C18H18N4O3S |
CAS No. | 1073485-20-7 |
Storage | 3 years -20℃Powder |
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6 months-80℃in solvent (DMSO, water, etc.) | |
Synonyms | LDC067 |
Solubility (25°C) * | In vitro | DMSO | 74 mg/mL (199.76 mM) |
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Water | <1 mg/mL ( | ||
Ethanol | <1 mg/mL ( | ||
* <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. |
Chemical Name | 3-[[6-(2-methoxyphenyl)-4-pyrimidinyl]amino]-benzenemethanesulfonamide |
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Группа Продуктов : Клеточный цикл > CDK ингибитор
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