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CAS No.: 1232410-49-9

VE-821 Catalog No. CSN15863

Synonyms: ATR Inhibitor IV

VE-821 is a potent and selective ATP competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 ATR

Ki:13nM
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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

更多
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7144 mL
- 13.5718 mL
- 27.1437 mL
- 5 mM
- 0.5429 mL
- 2.7144 mL
- 5.4287 mL
- 10 mM
- 0.2714 mL
- 1.3572 mL
- 2.7144 mL

技术信息

CAS号

1232410-49-9

储存条件

粉末: Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H16N4O3S

运输

蓝冰

分子量

368.41

别名

ATR Inhibitor IV

溶解度

DMSO	170.0 mg/mL (461.4 mM) warming
Water	insoluble

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

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