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CP-466722

现货
Catalog No.
A8625
ATM抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 1,000.00
Ship with 10-15 days
10mg
¥ 1,540.00
Ship with 10-15 days
50mg
¥ 4,240.00
Ship with 10-15 days

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Background

CP-466722 is a selective inhibitor of ATM kinase with IC50 value of 0.41 μM [1].

ATM (ataxia-telangiectasia, mutated) is a serine/threonine protein kinase and plays an important role in the cellular responses to DNA double-strand breaks (DSBs) [2] [3].

CP-466722 is a potent ATM inhibitor and is regareded as a promising drug to increase tumor cells sensitivity to IR. When tested with MCF7 cells, CP-466722 (10 μM) showed inhibition on the pATM and pKAP1 signals which induced by etoposide pre-treatment (25 μM) [1]. In GBM 12 cells, CP-466722 treatment significantly increased the cell sensitivity to TMZ and increased the cell apoptosis which had no effect on the TMZ-resistant GBM12 TMZ cells which indicated that CP-466722 (as an ATM inhibitor) may enhance the efficacy of TMZ in tumors that were inherently sensitive to TMZ [2]. When tested with Hela, MCF-7 and mouse cells pre-treated with IR which induced the increase in ATM-dependent phosphorylation events and then CP-466722 treatment resulted in the disruption of ATM-dependent phosphorylation events and inhibiton of ATM-dependent p53 inducetion at the minimal dose of 6 μM. Further, it was shown that CP-466722 treatment disrupted ATM-dependent cell cycle in increasing the percent in G2/M phase while decreasing the proportion in G1-phase without adverse effects [3].

References:
[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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt349.35
Cas No.1080622-86-1
FormulaC17H15N7O2
Solubility≥4.36mg/mL in DMSO with ultrasonic and warming
Chemical Name2-(6,7-dimethoxyquinazolin-4-yl)-5-pyridin-2-yl-1,2,4-triazol-3-amine
SDFDownload SDF
Canonical SMILESCOC1=C(C=C2C(=C1)C(=NC=N2)N3C(=NC(=N3)C4=CC=CC=N4)N)OC
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。

生物活性

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

质量控制和MSDS

批次:

化学结构

CP-466722