BMS-265246

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Chemical Structure| 582315-72-8 同义名 : -
CAS号 : 582315-72-8
货号 : A107996
分子式 : C18H17F2N3O2
纯度 : 99%+
分子量 : 345.343
MDL号 : MFCD22420825
存储条件：

Pure form Sealed in dry,2-8°C

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

DMSO: 12 mg/mL(34.75 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/CyclinD, IC50:230 nM

  • CDK2

    CDK2/CyclinE, IC50:9 nM

  • CDK1

    CDK1/CyclinB, IC50:6 nM
描述 Cyclin-dependent kinases (CDKs) are a family of protein kinases which along with their regulatory subunit cyclins play a key role in the growth, development, proliferation and death of eukaryotic cells and are responsible for insuring integrity in the coordination of events through the cell cycle[3]. BMS-265246 has been identified as a potent, selective inhibitor of CDK1 (IC50 = 0.006 μM) and CDK2 (IC50 = 0.009 μM) in vitro. In an ovarian cancer cell line (A2780) inhibitor BMS-265246 produced a cytotoxic effect with an IC50 = 0.76 μM[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.90mL

0.58mL

0.29mL

14.48mL

2.90mL

1.45mL

28.96mL

5.79mL

2.90mL
参考文献

[1]Sutherland JJ, Low J, Blosser W, Dowless M, Engler TA, Stancato LF. A robust high-content imaging approach for probing the mechanism of action and phenotypic outcomes of cell-cycle modulators. Mol Cancer Ther. 2011 Feb;10(2):242-54.

[2]Misra RN, Xiao Hy, et al. 1H-Pyrazolo[3,4-b] pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues. Bioorg Med Chem Lett. 2003 Jul 21;13(14):2405-8.

[3]Misra RN, Xiao Hy, Rawlins DB, Shan W, Kellar KA, Mulheron JG, Sack JS, Tokarski JS, Kimball SD, Webster KR. 1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues. Bioorg Med Chem Lett. 2003 Jul 21;13(14):2405-8. doi: 10.1016/s0960-894x(03)00381-0. PMID: 12824044.