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BMS265246 Sale

目录号 : GC12865

A cell-permeable inhibitor of Cdk1 and Cdk2

BMS265246 Chemical Structure

Cas No.:582315-72-8

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,439.00
现货
5mg
¥1,376.00
现货
10mg
¥1,901.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment [1]:

Cell lines

HCT-116 cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

0.293 ~ 0.492 μM

Applications

In HCT-116 cells, BMS265246 blocked the cell proliferation with EC50 values ranging from 0.293 to 0.492 μM. Compared with R-547 group, BMS265246 group had a higher proportion of G2-apoptotic cells. BMS265246 treatment resulted in low DNA intensity, large round nuclei and 4N DNA content in the dominant cell population-G2 arrested cells.

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.

产品描述

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

Cas No. 582315-72-8 SDF
化学名 (4-butoxy-1H-pyrazolo[3,4-b]pyridin-5-yl)-(2,6-difluoro-4-methylphenyl)methanone
Canonical SMILES CCCCOC1=C2C=NNC2=NC=C1C(=O)C3=C(C=C(C=C3F)C)F
分子式 C18H17F2N3O2 分子量 345.34
溶解度 ≥ 17.25mg/mL in DMSO 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.8957 mL 14.4785 mL 28.957 mL
5 mM 0.5791 mL 2.8957 mL 5.7914 mL
10 mM 0.2896 mL 1.4478 mL 2.8957 mL
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