SKI II
SKI II атрибут
Температура кипения: |
507.1±60.0 °C(Predicted) |
плотность: |
1.415±0.06 g/cm3(Predicted) |
RTECS: |
SK5900000 |
температура хранения: |
2-8°C |
растворимость: |
ДМСО: ≥20 мг/мл |
форма: |
Твердый |
пка: |
10.17±0.26(Predicted) |
цвет: |
От белого |
Чувствительный: |
Air & Light Sensitive |
Справочник по базе данных CAS: |
312636-16-1 |
безопасность
- Заявления о рисках и безопасности
- код информации об опасности(GHS)
символ(GHS) |
|
сигнальное слово |
Warning |
Заявление об опасности |
пароль |
Заявление об опасности |
Класс опасности |
категория |
сигнальное слово |
пиктограмма |
предупреждение |
H302 |
Вредно при проглатывании. |
Острая токсичность, пероральная |
Категория 4 |
Предупреждение |
![](/GHS07.jpg) |
P264, P270, P301+P312, P330, P501 |
|
Внимание |
P280 |
Использовать перчатки/ средства защиты глаз/ лица. |
P305+P351+P338 |
ПРИ ПОПАДАНИИ В ГЛАЗА: Осторожно промыть глаза водой
в течение нескольких минут. Снять контактные линзы, если
Вы ими пользуетесь и если это легко сделать. Продолжить
промывание глаз. |
|
SKI II химические свойства, назначение, производство
Использование
SKI II is a nonlipid inhibitor of sphingosine kinase. SKI II s orally bioavailable and has shown significant inhibition of tumor growth in mice.
Биологическая активность
Selective non-lipid inhibitor of sphingosine kinase (IC 50 = 0.5 μ M); does not act at ATP-binding site. Displays no inhibition of ERK2, PI 3-kinase, or PKC α at concentrations up to 60 μ M. Reduces levels of sphingosine-1-phosphate in MDA-MB-231 breast cancer cells. Induces apoptosis and inhibits proliferation in several other tumor cell lines in vitro (IC 50 = 0.9-4.6 μ M).
Биохимия/физиол Действия
Sphingosine kinase (SK) plays a pivotal role in regulating tumor growth and SK can act as an oncogene. Expression of SK RNA is significantly elevated in a variety of solid tumors, compared with normal tissue from the same patient. A number of novel inhibitors of human SK were identified, and several representative compounds were characterized in detail. These compounds demonstrated activity at sub- to micromolar concentrations, making them more potent than any other reported SK inhibitor, and were selective toward SK compared with a panel of human lipid and protein kinases. Kinetic studies revealed that the compounds were not competitive inhibitors of the ATP-binding site of SK. 4-[4-(4-chloro-phenyl)-thiazol-2-ylamino]-phenol (SKI-II) inhibitor is orally bioavailable, detected in the blood for at least 8 h, and showed a significant inhibition of tumor growth in mice with IC50 = 0.5 μM; SKI II does not act at ATP-binding site. Displays no inhibition of ERK2, PI 3-kinase, or PKCa at concentrations up to 60 μM.SKI II induces apoptosis and inhibits proliferation in several other tumor cell lines in vitro (IC50 = 0.9-4.6 μM).
SKI II препаратная продукция и сырье
сырьё
препарат
SKI II поставщик
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312636-16-1()подобный поиск: