R547

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Chemical Structure| 741713-40-6 同义名 : Ro 4584820
CAS号 : 741713-40-6
货号 : A454118
分子式 : C18H21F2N5O4S
纯度 : 99%+
分子量 : 441.452
MDL号 : MFCD09970629
存储条件：

Pure form Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(237.85 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • CDK4

    CDK4/CyclinD1, Ki:1 nM

  • CDK2

    CDK2/CyclinE, Ki:3 nM

  • CDK1

    CDK1/CyclinB, Ki:2 nM
描述 R547 is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2 nM/3 nM/1 nM.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.27mL

0.45mL

0.23mL

11.33mL

2.27mL

1.13mL

22.65mL

4.53mL

2.27mL
参考文献

[1]DePinto W, Chu XJ, et al. In vitro and in vivo activity of R547: a potent and selective cyclin-dependent kinase inhibitor currently in phase I clinical trials. Mol Cancer Ther. 2006 Nov;5(11):2644-58.

[2]Chu XJ, DePinto W, et al. Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl] (2,3-difluoro-6- methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity. J Med Chem. 2006 Nov 2;49(22):6549-60.