2. Cell Cycle/DNA Damage PI3K/Akt/mTOR
  3. ATM/ATR
  4. VE-821

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

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VE-821 Chemical Structure

VE-821 Chemical Structure

CAS No. : 1232410-49-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥550
In-stock
1 mg ￥250
In-stock
5 mg ￥500
In-stock
10 mg ￥850
In-stock
25 mg ￥1500
In-stock
50 mg ￥2500
In-stock
100 mg ￥4500
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

VE-821 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 40 篇科研文献

WB
Proliferation Assay

    VE-821 purchased from MCE. Usage Cited in: Eur J Med Chem. 2017 Feb 15;127:691-702.  [Abstract]

    Relative cell viability (%) in MDCK CAIX- and CAIX+ cells exposed to ATR inhibitors (VE-821 and VE-822) or the CAIXi conjugated derivatives in combination with radiation during normoxia (21% O2) and anoxia (≤0.02% O2). Normoxic cells are irradiated with 2 Gy and anoxic cells with 4 Gy to induce similar effects on cell viability.

    VE-821 purchased from MCE. Usage Cited in: Front Oncol. 2017 May 19;7:98.  [Abstract]

    ATM inhibition by treatment with KU-55933 (10 µM) strongly reduces HR efficiency in JJN3-HR and U266-HR, although cells are still able to perform HR to some extent.

    VE-821 purchased from MCE. Usage Cited in: Oncogene. 2016 Sep 8;35(36):4689-97.  [Abstract]

    Western blotting analysis of lysates from λ820 cells treated with vehicle (0.1% DMSO), 10 μM of the ATR inhibitor VE-821, 1 μM of ATR inhibitor AZ20, 1 μM PI3K/mTOR inhibitor NVP-BEZ235 or indicated concentrations of PI3K/mTOR inhibitor GSK1059615.

    VE-821 purchased from MCE. Usage Cited in: DNA Repair (Amst). 2016 Apr;40:35-46.  [Abstract]

    Impact of ATR inhibition on DNA damage response, γ-H2Ax foci formation and cytotoxicity: A representative immunoblot with vinculin used as a loading control(A) shows the impact of ATR inhibition (VE-821) on the early (0.5 h) and late (24 h) DDR to the indicated treatments in H460 cells. pATM fold change shown above the immunoblot (A).

    VE-821 purchased from MCE. Usage Cited in: Sahlgrenska Academy. University of Gothenburg. 2016 Mar.

    ATRi (VE821) reduces the phosphorylation of CHK1, but not of 4EBP1 or S6, validating our hypothesis.

    查看 ATM/ATR 亚型特异性产品:

    查看所有亚型
    ATM ATR

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

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

    IC50 & Target[1]

    ATR

    13 nM (Ki)

    ATM

    16 μM (Ki)

    DNA-PK

    2.2 μM (Ki)

    PI3Kγ

    3.9 μM (Ki)

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    K562 ED50
    448.883 μM
    Compound: 7; VE-821
    Cytotoxicity against human K562 cells assessed as decrease in cell viability after 24 hrs by cell titer-glo luminescence assay
    Cytotoxicity against human K562 cells assessed as decrease in cell viability after 24 hrs by cell titer-glo luminescence assay
    		[PMID: 27177826]
    K562 ED50
    71 μM
    Compound: 7; VE-821
    Cytotoxicity against human K562 cells assessed as decrease in cell viability after 48 hrs by cell titer-glo luminescence assay
    Cytotoxicity against human K562 cells assessed as decrease in cell viability after 48 hrs by cell titer-glo luminescence assay
    		[PMID: 27177826]
    体外研究
    (In Vitro)

    VE-821 对 ATR 具有极好的选择性，对相关 PIKK ATM、DNA-PK、mTOR 和 PI3Kγ（Ki 值分别为 16 μM、2.2 μM、>1 μM 和 3.9 μM）以及一大批不相关的蛋白激酶的交叉反应性极小[1]。VE-821 还抑制 ATM 和 DNA-PK，IC50 值分别为 >8 μM 和 4.4 μM[2]。VE-821 显著增强了 PSN-1、MiaPaCa-2 和原发性 PancM 胰腺癌细胞在常氧和缺氧条件下对放射和吉西他滨的敏感性。 VE-821 抑制 ATR 可抑制癌细胞中辐射诱导的 G2/M 停滞。在 PSN-1 和 MiaPaCa-2 细胞中，在用吉西他滨 (100 nM)、辐射 (6 Gy) 或两者处理后，在辐射后 2 小时，1 μM VE-821 可抑制 Chk1 (Ser 345) 的磷酸化[3]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    VE-821 相关抗体:
    分子量

    368.41

    Formula

    C18H16N4O3S
    CAS 号
    性状

    固体

    颜色

    Light green to green

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 50 mg/mL (135.72 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制储备液
    浓度 溶剂体积 质量 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
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验：

    以下溶解方案源自文献，仅供参考，建议您先取少量样品进行尝试。

    • 方案 一

      VE-821 is prepared im vehicle (10% PEG300, 2.5% Tween-80, pH 4)[4].

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    纯度 & 产品资料
    参考文献
    Kinase Assay
    [2]

    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[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [3]

    MiaPaCa-2, PSN-1 and Panc1 cells (5×104) are plated in 96-well plates and after 4 h treated with increasing concentrations of VE-821 at 1 h before irradiation with a single dose of 4 Gy. Medium is replaced 72 h post-irradiation at which point viability is measured using the using the Alamar Blue assay. Cells are allowed to proliferate and cell viability is again analyzed at day 10 for the different treatment conditions. Cell viability and surviving fraction are normalized to the untreated (control) group[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    参考文献

    VE-821 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    可选溶剂 浓度 溶剂体积 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
    15 mM 0.1810 mL 0.9048 mL 1.8096 mL 4.5239 mL
    20 mM 0.1357 mL 0.6786 mL 1.3572 mL 3.3930 mL
    25 mM 0.1086 mL 0.5429 mL 1.0857 mL 2.7144 mL
    30 mM 0.0905 mL 0.4524 mL 0.9048 mL 2.2620 mL
    40 mM 0.0679 mL 0.3393 mL 0.6786 mL 1.6965 mL
    50 mM 0.0543 mL 0.2714 mL 0.5429 mL 1.3572 mL
    60 mM 0.0452 mL 0.2262 mL 0.4524 mL 1.1310 mL
    80 mM 0.0339 mL 0.1696 mL 0.3393 mL 0.8482 mL
    100 mM 0.0271 mL 0.1357 mL 0.2714 mL 0.6786 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    VE-8211232410-49-9VE821VE 821ATM/ATRAtaxia telangiectasia mutatedATM and RAD3 relatedInhibitorinhibitorinhibit

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