BMS265246
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
BMS265246是一种强效的和选择性的CDK1和CDK2抑制剂(IC50= 6 nM和9 nM).
细胞周期蛋白依赖性激酶(CDK)是一组丝氨酸/苏氨酸激酶.他们通过与细胞周期蛋白耦合而被激活,参与调节细胞周期.
BMS265246抑制Cdk4/cycD活性,阻止A2780 Cytox (IC50 = 0.23 μM和0.76 μM) [1].在HCT-116细胞中,BMS-265246抑制细胞增殖(EC50= 0.293 μM-0.492 μM).BMS-265246用药后,在主导细胞群,即G2期阻滞细胞中观察到低DNA密度,细胞核大而圆及4N DNA的含量[2].
参考文献:
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.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 345.34 |
Cas No. | 582315-72-8 |
Formula | C18H17F2N3O2 |
Solubility | insoluble in H2O; insoluble in EtOH; ≥17.25 mg/mL in DMSO |
Chemical Name | (4-butoxy-1H-pyrazolo[3,4-b]pyridin-5-yl)-(2,6-difluoro-4-methylphenyl)methanone |
SDF | Download SDF |
Canonical SMILES | CCCCOC1=C2C=NNC2=NC=C1C(=O)C3=C(C=C(C=C3F)C)F |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
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. |
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 |