GW5074 220904-83-6
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 520.94 GW5074 - мощный и селективный ингибитор c-Raf с IC50 9 нМ, не влияет на активность JNK1 / 2/3, MEK1, MKK6 / 7, Отмечены CDK1 / 2, c-Src, p38 MAP, VEGFR2 или c-Fms. \ N Биологическая активность Протокол (только для справки) Анализ киназы: [1]
Клеточный анализ: [1]
Исследование на животных: [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
Affinity determination | In general, in vitro kinase assays are performed using purified kinase and synthetic substrates under standard conditions using the Kinase Profiling service of Upstate Biotechnology. Briefly, for each assay 5–10 mU of purified kinase is used. For GSK3β, cdk1, cdk2, cdk3, cdk5, the kinase is incubated with 1 μM GW5074 in a buffer containing 8 mM MOPS, pH 7.2, 0.2 mM EDTA, 10 mM magnesium acetate and [c- 33P-ATP] for 40 min at room temperature. Kinase activity is quantified by measuring 33P incorporation by spotting an aliquot on P30 filters, washing in 50 mM phosphoric acid and scintillation counting. The buffer composition for c-Raf, JNK1, JNK2, JNK3, MEK1, MKK6, MKK7 is 50 mM Tris pH 7.5, 0.1 mM EGTA, 10 mM magnesium acetate and [c- 33P-ATP]. The peptide substrates used are as follows: For c-Raf, 0.66 mg/mL MBP; for cdks, 0.1 mg/mL histone H1; for JNKs, 3 μM ATF2; for MEK1, 1 μM MAPK2; for MKK6, 1 μM of SAPK2a and for MKK7, 2 μM JNK1α. |
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Cell lines | Cortical neurons |
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Concentrations | ~5 μM |
Incubation Time | 24 hours |
Method | HCA is diluted from 100-fold concentrated solutions that are adjusted to pH 7.5. To evaluate the effects of GW5074 on HCA-induced cytotoxicity, GW5074 is added at the time cortical neurons are exposed to HCA. Viability is assessed 24 h later. |
Animal Models | Eight-week-old C57BL/6 male mice administered with 50–55 mg/kg 3-NP | ||
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Formulation | In saline | ||
Dosages | 0.5–10 mg/kg | ||
Administration | i.p. | ||
Solubility | 30% propylene glycol, 5% Tween 80, 65% D5W, 30 mg/mL | ||
* 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. |
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) | 520.94 |
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Formula |
C15H8Br2INO2 |
CAS No. | 220904-83-6 |
Storage | 3 years -20℃Powder |
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6 months-80℃in solvent (DMSO, water, etc.) | |
Synonyms |
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Solubility (25°C) * | In vitro | DMSO | 104 mg/mL (199.63 mM) |
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Water | <1 mg/mL ( | ||
Ethanol | <1 mg/mL ( | ||
In vivo | 30% propylene glycol, 5% Tween 80, 65% D5W | 30 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 | 2H-Indol-2-one, 3-[(3,5-dibromo-4-hydroxyphenyl)methylene]-1,3-dihydro-5-iodo- |
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Группа Продуктов : MAPK > Раф ингибитор
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