VE-821

产品说明书

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Chemical Structure| 1232410-49-9 同义名 : ATR Inhibitor IV
CAS号 : 1232410-49-9
货号 : A312952
分子式 : C18H16N4O3S
纯度 : 99%+
分子量 : 368.41
MDL号 : MFCD19443686
存储条件：

Pure form Keep in dark place,Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(135.72 mM)，配合低频超声助溶，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：

IP 2% DMSO+2% Tween80+40% PEG300+water 1.7 mg/mL clear

PO 0.5% CMC-Na 20 mg/mL suspension

生物活性
靶点

  • ATR

    ATR, Ki:13 nM
描述 ATR/ATM kinases can phosphorylate a broad and overlapping catalogue of several thousand substrates in DNA damage signaling. The kinase activity of ATR, activated by single-stranded DNA (ssDNA) coated with replication protein A (RPA), is increased at damaged replication forks and resected DNA double-strand breaks (DSBs). VE-821 is a potent and selective ATR inhibitor with Ki value of 13nM. Pre-treatment with 10μM inhibited the H2AX phosphorylation at an early time point after exposure to the S phase poisons cisplatin and gemcitabine, but not the double-strand breaks inducers etoposide and ionizing radiation in HFL1 cells, suggesting the selective inhibition on ATR by VE-821. It showed strong synergy with genotoxic agents from multiple classes, most marked with cisplatin and carboplatin, in HCT116 cancer cells, but not in normal cell lines. In addition, cisplatin and VE-821 clearly acted synergistically in the ATM-null cells but not in the normal cells, indicating the reliance on ATR for survival from DNA damage in cancer cells with defects in ATM signaling[1].
作用机制 VE-821 is a potent ATP-competitive inhibitor of ATR.[1]
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
CAL72 Growth Inhibition Assay IC50～0.8 μM 25593184
HCT-116 p53-/- 1/3/10 μM Cytotoxicity Assay 1 h potentiates the cytotoxicity of both camptothecin and LMP-400 25269479
HCT-116 p53+/+ 1/3/10 μM Cytotoxicity Assay 1 h potentiates the cytotoxicity of both camptothecin and LMP-400 25269479
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.71mL

0.54mL

0.27mL

13.57mL

2.71mL

1.36mL

27.14mL

5.43mL

2.71mL
参考文献

[1]Reaper PM, Griffiths MR, et al. Selective killing of ATM- or p53-deficient cancer cells through inhibition of ATR. Nat Chem Biol. 2011 Apr 13;7(7):428-30.