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CGK733

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Chemical Structure| 905973-89-9 同义名 : ATM/ATR Kinase Inhibitor
CAS号 : 905973-89-9
货号 : A140835
分子式 : C23H18Cl3FN4O3S
纯度 : 99%+
分子量 : 555.836
MDL号 : MFCD09038682
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(188.9 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • ATM

    ATM, IC50:200 nM

  • ATR

    ATR, IC50:200 nM
描述 The ataxia telangiectasia mutated (ATM) and ATM-related (ATR) kinases facilitate the resistance of cancer cells to genotoxic agents. CGK733 is a thiourea-containing compound that inhibits both ATM and ATR with IC50 values of ~200nM. Treatment of MCF-7 breast cancer cells with 10μM CGK733 reduced the expression of cyclin D1 within 2h of exposure. CGK733 at 5-20μM induced a loss of cyclin D1 protein in T47D cells. In MCF-7 cells, treatment with CGK733 at 10μM for 24h reduced the expression of both phosphorylated and total retinoblastoma tumor suppressor protein. CGK733 at a dosage of 10μM inhibited the proliferation of MCF-7, T47D, HCT116, BALB/c3T3, MDA-MB436, and LnCap cancer cells.[3] In mice inoculated with D54-ATMR cells, treatment with CGK733 (25mg/kg) for 1, 4, and 8h induced an increase in ATM reporter activity with 2.4-fold, 3.1-fold, and 1.3-fold changes, respectively, over the control group.[4]
作用机制 CGK733 is a small-molecule inhibitor of both ATM and ATR.[3]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.80mL

0.36mL

0.18mL

9.00mL

1.80mL

0.90mL

17.99mL

3.60mL

1.80mL
参考文献

[1]Wang Y, Kuramitsu Y, et al. CGK733-induced LC3 II formation is positively associated with the expression of cyclin-dependent kinase inhibitor p21Waf1/Cip1 through modulation of the AMPK and PERK/CHOP signaling pathways. Oncotarget. 2015 Nov 24;6(37):39692-701.

[2]Crescenzi E, Palumbo G, et al. Ataxia telangiectasia mutated and p21CIP1 modulate cell survival of drug-induced senescent tumor cells: implications for chemotherapy. Clin Cancer Res. 2008 Mar 15;14(6):1877-87.

[3]Alao JP, Sunnerhagen P. The ATM and ATR inhibitors CGK733 and caffeine suppress cyclin D1 levels and inhibit cell proliferation. Radiat Oncol. 2009;4:51. Published 2009 Nov 10. doi:10.1186/1748-717X-4-51

[4]Williams TM, Nyati S, Ross BD, Rehemtulla A. Molecular imaging of the ATM kinase activity. Int J Radiat Oncol Biol Phys. 2013;86(5):969-977. doi:10.1016/j.ijrobp.2013.04.028