Name: CP-466722
Price: 276.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    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].
    
    [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.
- Properties
  - Alternative Name
    
    2-(6,7-dimethoxyquinazolin-4-yl)-5-pyridin-2-yl-1,2,4-triazol-3-amine
    
    CAS Number
    
    1080622-86-1
    
    Molecular Formula
    
    C17H15N7O2
    
    Molecular Weight
    
    349.35
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥4.36 mg/mL in DMSO with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

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