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

VE-821 是一種有效的 ATP 競爭性的 ATR 抑制劑，Ki/IC50 為 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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規(guī)格 價格 是否有貨 數(shù)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   詢價  
500 mg   詢價  

* Please select Quantity before adding items.

Customer Review

MCE 顧客使用本產品發(fā)表的 40 篇科研文獻

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 亞型特異性產品:

    • 生物活性

    • 實驗參考方法

    • 純度 & 產品資料

    • 參考文獻

    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)

    細胞效力
    (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]
    體外研究
    (In Vitro)

    VE-821 對 ATR 具有極好的選擇性，對相關 PIKK ATM、DNA-PK、mTOR 和 PI3Kγ（Ki 值分別為 16 μM、2.2 μM、>1 μM 和 3.9 μM）以及一大批不相關的蛋白激酶的交叉反應性極小[1]。VE-821 還抑制 ATM 和 DNA-PK，IC50 值分別為 >8 μM 和 4.4 μM[2]。VE-821 顯著增強了 PSN-1、MiaPaCa-2 和原發(fā)性 PancM 胰腺癌細胞在常氧和缺氧條件下對放射和吉西他濱的敏感性。 VE-821 抑制 ATR 可抑制癌細胞中輻射誘導的 G2/M 停滯。在 PSN-1 和 MiaPaCa-2 細胞中，在用吉西他濱 (100 nM)、輻射 (6 Gy) 或兩者處理后，在輻射后 2 小時，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.
    分子量

    368.41

    Formula

    C18H16N4O3S
    CAS 號
    性狀

    固體

    顏色

    Light green to green

    運輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性數(shù)據(jù)
    細胞實驗： 

    DMSO 中的溶解度 : 50 mg/mL (135.72 mM; 超聲助溶; 吸濕的 DMSO 對產品的溶解度有顯著影響，請使用新開封的 DMSO)

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

    配制儲備液
    濃度 溶劑體積 質量 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
    查看完整儲備液配制表

    * 請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
    儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲存時，請在1年內使用， -20°C儲存時，請在6個月內使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實驗：

    以下溶解方案源自文獻，僅供參考，建議您先取少量樣品進行嘗試。

    • 方案 一

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

    動物溶解方案計算器
    請輸入動物實驗的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實驗過程有損耗，建議您多配一只動物的量
    計算結果
    工作液所需濃度 : mg/mL
    純度 & 產品資料
    參考文獻
    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.
    參考文獻

    完整儲備液配制表

    * 請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
    儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲存時，請在1年內使用， -20°C儲存時，請在6個月內使用。

    可選溶劑 濃度 溶劑體積 質量 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.

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    產品名稱：
    VE-821
    目錄號：
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