[4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone(R 547)
[4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone(R 547) атрибут
Температура кипения: |
703.7±70.0 °C(Predicted) |
плотность: |
1.49 |
температура хранения: |
Store at -20°C |
растворимость: |
Растворим в ДМСО |
форма: |
Кристаллическое твердое вещество |
пка: |
4.22±0.10(Predicted) |
цвет: |
White to off-white |
FDA UNII: |
T61871RKRI |
Заявления о рисках и безопасности
[4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone(R 547) химические свойства, назначение, производство
Описание
Cyclin-dependent kinases (Cdks) are critical positive regulators of cell cycle progression and cellular transcription whose dysregulation can lead to the development of cancer. R547 is a diaminopyrimidine compound that inhibits Cdk1/cyclin B, Cdk2/cyclin E, and Cdk4/cyclin D1 (Kis = 1-3 nM). It is inactive against a panel of more than 120 unrelated kinases (Kis > 5 μM). R547 inhibits tumor cell proliferation (IC50s ≤ 0.6 μM in vitro), inducing cell cycle arrest at G1 and G2 phases and apoptosis as well as reducing phosphorylation of the retinoblastoma protein. It also demonstrates antitumor activity in vivo in various human tumor xenograft models.
[4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone(R 547) препаратная продукция и сырье
сырьё
препарат
[4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone(R 547) поставщик
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