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BMS265246

现货
Catalog No.
A8385
CDK1/2抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 2,090.00
Ship with 10-15 days
5mg
¥ 1,890.00
现货
10mg
¥ 2,590.00
现货

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Background

BMS265246 is a potent and selective inhibitor for CDK1 and CDK2 (IC50= 6 nM and 9 nM)

Cyclin-dependent kinases (CDK) are a group of serine/threonine kinases. They are activated by coupling to cyclin and participate in the regulation of cell cycle.

BMS265246 inhibited the Cdk4/cycD activity and prevented A2780 Cytox (IC50 = 0.23 μM and 0.76 μM) [1]. In HCT-116 cells, BMS-265246 blocked the cell proliferation (EC50= 0.293 μm—0.492 μm). Following the treatment of BMS-265246, low DNA intensity, large round nuclei and 4N DNA content were observed in the dominant cell population –G2 arrested cells. [2]

References:
1. Misra RN, Xiao Hy, Rawlins DB 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.
2. Sutherland JJ, Low J, Blosser W et al.  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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt345.34
Cas No.582315-72-8
FormulaC18H17F2N3O2
Solubility≥17.25mg/mL in DMSO
Chemical Name(4-butoxy-1H-pyrazolo[3,4-b]pyridin-5-yl)-(2,6-difluoro-4-methylphenyl)methanone
SDFDownload SDF
Canonical SMILESCCCCOC1=C2C=NNC2=NC=C1C(=O)C3=C(C=C(C=C3F)C)F
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

HCT-116细胞

制备方法

在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

0.293 ~ 0.492 μM

实验结果

在HCT-116细胞中,BMS265246阻断细胞增殖,其EC50值为0.293 ~ 0.492 μM。与R-547组相比,BMS265246组具有较高比例的G2凋亡细胞。经BMS265246治疗后,主要细胞群(即G2阻滞细胞)具有较低的DNA密度、大圆核以及4N DNA。

References:

[1]. Sutherland JJ, Low J, Blosser W et al. 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.

生物活性

Description BMS-265246是一种强效的和选择性的CDK1 和 CDK2抑制剂,IC50值分别为6 nM 和9 nM.
靶点 CDK1/CyclinB CDK2/CyclinE CDK4/CyclinD      
IC50 6 nM 9 nM 230 nM      

质量控制

质量控制和MSDS

批次:

化学结构

BMS265246