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VE-821

产品编号 T3032 CAS 1232410-49-9

别名: ATR Inhibitor IV

VE-821 (ATR Inhibitor IV) 是一种有效的 ATP 竞争性的ATR 抑制剂，Ki 为 13 nM，IC50为 26 nM。

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VE-821, CAS 1232410-49-9

规格	价格/CNY	货期
5 mg	￥ 415	现货
10 mg	￥ 697	现货
25 mg	￥ 1,259	现货
50 mg	￥ 1,996	现货
100 mg	￥ 3,717	现货
1 mL * 10 mM (in DMSO)	￥ 457	现货

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	VE-821 (ATR Inhibitor IV) is a selective ATP competitive inhibitor of ATR( Ki/IC50: 13/26 nM in cell-free assays).
靶点活性	ATR:13 nM (Ki, cell free)
体外活性	VE-821 shows excellent selectivity for ATR with minimal cross-reactivity against the related PIKKs ATM, DNA-dependent protein kinase (DNA-PK), mammalian target of rapamycin and phosphoinositol 3-kinase-γ (Kis of 16 μM, 2.2 μM, >1 μM and 3.9 μM, respectively). VE-821 blocked H2AX phosphorylation in hydroxyurea-treated HT29 cancer cells and had no impact on the M059J or HT144 lines treated with neocarzinostatin [1]. VE-821 significantly enhanced the sensitivity of PSN-1, MiaPaCa-2 and primary PancM pancreatic cancer cells to radiation and gemcitabine under both normoxic and hypoxic conditions. ATR inhibition by VE-821 led to inhibition of radiation-induced G 2/M arrest in cancer cells [2]. VE-821 (1 and 4 μM) enhanced H2AX phosphorylation on Ser139 induced by topotecan, and cisplatin in OVCAR-8 cells. VE-821 did not block ATR-mediated Ser345 Chk1 or Ser296 autophosphorylation triggered by gemcitabine, topotecan, or cisplatin [3].
激酶实验	The ability of compounds (e.g., VE-821) to inhibit ATR, ATM or DNAPK kinase activity is tested using a radiometric-phosphate incorporation assay. A stock solution is prepared consisting of the appropriate buffer, kinase, and target peptide. To this is added the compound of interest, at varying concentrations in DMSO to a final DMSO concentration of 7%. Assays are initiated by addition of an appropriate [g-33P]ATP solution and incubated at 25°C. Assays are stopped, after the desired time course, by addition of phosphoric acid and ATP to a final concentration of 100 mM and 0.66 μM, respectively. Peptides are captured on a phosphocellulose membrane, prepared, and washed six times with 200 μL of 100 mM phosphoric acid, prior to the addition of 100 μL of scintillation cocktail and scintillation counting on a 1450 Microbeta Liquid Scintillation Counter. Dose-response data are analyzed using GraphPad Prism software [4].
细胞实验	Clonogenic survival assays were performed as described before. Briefly, logarithmically growing cells were plated in triplicate in 6-well tissue culture dishes under oxic (21% O2) or hypoxic conditions (0.5% O2) using an InVivo2 300 chamber. Cells were incubated for 6 h before irradiation under oxia or hypoxia using tightly sealed chambers. The target O2 level was achieved within 6 h of gassing and maintained during irradiation, as confirmed by an OxyLite oxygen probe. Cells irradiated under hypoxia were exposed to normoxia at 1 h post-irradiation. As standard, VE-821 (1 μM) was added 1 h prior to irradiation (6 Gy) and was washed away 72 h after irradiation. For the chemotherapy experiments, cells were initially exposed to increasing concentrations of gemcitabine (5, 10 and 20 nM) for 24 h before addition of the VE-821 (1 μM) for another 72 h. The effect of triple combination of irradiation with VE-821 and gemcitabine was examined as well. Cells were incubated for 10–21 d until colonies were stained with 0.5% crystal violet and counted in a CellCount automated colony counter. Clonogenic survival was calculated and data were fitted in GraphPad Prism 4.0 [2].

别名	ATR Inhibitor IV
分子量	368.41
分子式	C18H16N4O3S
CAS No.	1232410-49-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 69 mg/mL (187.3 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7144 mL	13.5718 mL	27.1437 mL	67.8592 mL
	5 mM	0.5429 mL	2.7144 mL	5.4287 mL	13.5718 mL
	10 mM	0.2714 mL	1.3572 mL	2.7144 mL	6.7859 mL
	20 mM	0.1357 mL	0.6786 mL	1.3572 mL	3.393 mL
	50 mM	0.0543 mL	0.2714 mL	0.5429 mL	1.3572 mL
	100 mM	0.0271 mL	0.1357 mL	0.2714 mL	0.6786 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

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参考文献

1. Reaper PM, 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. 2. Prevo R, et al. The novel ATR inhibitor VE-821 increases sensitivity of pancreatic cancer cells to radiation and chemotherapy. Cancer Biol Ther. 2012 Sep;13(11):1072-81. 3. Huntoon CJ, et al. ATR inhibition broadly sensitizes ovarian cancer cells to chemotherapy independent of BRCA status. Cancer Res. 2013 Jun 15;73(12):3683-91. 4. Charrier JD, et al. Discovery of potent and selective inhibitors of ataxia telangiectasia mutated and Rad3 related (ATR) protein kinase as potential anticancer agents. J Med Chem. 2011 Apr 14;54(7):2320-30. 5. Flach J, Jann J C, Knaflic A, et al. Replication stress signaling is a therapeutic target in myelodysplastic syndromes with splicing factor mutations[J]. Haematologica. 2020 6. Weizhe Li, Hong-Yan Wang, Xiaolu Zhao, Hongguo Duan, Binghua Cheng, Yafei Liu, Mengjie Zhao et al. A methylation-phosphorylation switch determines Plk1 kinase activity and function in DNA damage repair [J]. Science Advances. 2019 Mar 6;5(3):eaau7566. 7. Bai Y, Wang W, Li S, et al. C1QBP Promotes Homologous Recombination by Stabilizing MRE11 and Controlling the Assembly and Activation of MRE11/RAD50/NBS1 Complex[J]. Molecular Cell. 2019.

文献引用

1. Bai Y, Wang W, Li S, et al. C1QBP Promotes Homologous Recombination by Stabilizing MRE11 and Controlling the Assembly and Activation of MRE11/RAD50/NBS1 Complex. Molecular Cell. 2019 2. Li W, Wang H Y, Zhao X, et al. A methylation-phosphorylation switch determines Plk1 kinase activity and function in DNA damage repair. Science Advances. 2019, 5(3): eaau7566 3. Flach J, Jann J C, Knaflic A, et al. Replication stress signaling is a therapeutic target in myelodysplastic syndromes with splicing factor mutations. Haematologica. 2021 Nov 1;106(11):2906-2917

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

VE-821 1232410-49-9 DNA Damage/DNA Repair PI3K/Akt/mTOR signaling ATM/ATR ATM and RAD3 related VE 821 Inhibitor Ataxia telangiectasia mutated inhibit ATR Inhibitor IV VE821 inhibitor

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VE-821

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溶解度

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参考文献

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剂量换算

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