CP-466722
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.
CP-466722是ATM激酶的选择性抑制剂,其IC50值为0.41 μM[1]。
ATM(共济失调毛细血管扩张症突变蛋白)是一种丝氨酸/苏氨酸蛋白激酶,在细胞对DNA双链断裂(DSBs)的反应中起重要作用[2][3]。
CP-466722是一种有效的ATM抑制剂,有望成为增加肿瘤细胞对红外辐射敏感性的药物。在MCF7细胞中,10 μM的CP-466722可抑制Etoposide(25 μM)诱导的pATM和pKAP1信号[1]。在GBM12细胞中,CP-466722治疗显著增加细胞对TMZ的敏感性,促进细胞凋亡,但对TMZ抗性的GBM12 TMZ细胞没有影响,这表明CP-466722(作为一种ATM抑制剂)可增强TMZ对TMZ敏感性肿瘤的疗效[2]。在Hela细胞、MCF-7细胞和小鼠细胞中,预先用红外辐射处理,从而诱导ATM依赖性的磷酸化过程,CP-466722在6 μM的最小剂量时导致ATM依赖性磷酸化过程紊乱,抑制ATM依赖性的p53诱导。另外,实验表明,CP-466722可扰乱ATM依赖的细胞周期,增加处于G2/M期的细胞比例,同时减少处于G1期的细胞比例,而没有不利效应[3]。
参考文献:
[1]. Guo, K., et al., Development of a cell-based, high-throughput screening assay for ATM kinase inhibitors. J Biomol Screen, 2014. 19(4): p. 538-46.
[2]. Nadkarni, A., et al., ATM inhibitor KU-55933 increases the TMZ responsiveness of only inherently TMZ sensitive GBM cells. J Neurooncol, 2012. 110(3): p. 349-57.
[3]. Rainey, M.D., et al., Transient inhibition of ATM kinase is sufficient to enhance cellular sensitivity to ionizing radiation. Cancer Res, 2008. 68(18): p. 7466-74.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 349.35 |
Cas No. | 1080622-86-1 |
Formula | C17H15N7O2 |
Solubility | ≥4.36 mg/mL in DMSO with gentle warming and ultrasonic; insoluble in EtOH; insoluble in H2O |
Chemical Name | 2-(6,7-dimethoxyquinazolin-4-yl)-5-pyridin-2-yl-1,2,4-triazol-3-amine |
SDF | Download SDF |
Canonical SMILES | COC1=C(C=C2C(=C1)C(=NC=N2)N3C(=NC(=N3)C4=CC=CC=N4)N)OC |
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。 |
描述 | CP-466722是一种强效的和可逆的ATM抑制剂。 | |||||
靶点 | ATM | |||||
IC50 | 0.41 μM |
质量控制和MSDS
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