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

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

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CAS 番号 : 1232410-49-9

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10 mg $94 在庫あり
25 mg $165 在庫あり
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カスタマーレビュー

Based on 55 publication(s) in Google Scholar

VE-821 関連抗体

Top Publications Citing Use of Products

顧客検証

Cell Proliferation/Viability Assay
WB

    VE-821 purchased from MedChemExpress. 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. Cells were exposed to 500 nM VE-821 and 12, and to 50 nM VE-822 and 13.

    VE-821 purchased from MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. Usage Cited in: DNA Repair. 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 MedChemExpress. 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.

    ATM/ATR アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    ATM ATR TRRAP

    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    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)

    Cellular Effect
    Cell Line Type Value Description References
    K562 ED50
    448.883 3
    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
    448.883 3
    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 3
    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]
    K562 ED50
    71 3
    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]
    K562 ED50
    448.883 3
    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 3
    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]
    体外実験

    VE-821 shows excellent selectivity for ATR with minimal cross-reactivity against the related PIKKs ATM, DNA-PK, mTOR and PI3Kγ (Kis of 16 μM, 2.2 μM, >1 μM and 3.9 μM, respectively) and against a large panel of unrelated protein kinases[1]. VE-821 (compound 27) also inhibits ATM and DNA-PK wirh IC50 of >8 μM, and 4.4 μM, respectively[2]. VE-821 significantly enhances 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 leads to inhibition of radiation-induced G2/M arrest in cancer cells. In both PSN-1 and MiaPaCa-2 cells, 1 μM VE-821 inhibits phosphorylation of Chk1 (Ser 345) after treatment with Gemcitabine (100 nM), radiation (6 Gy) or both, at 2 h post-irradiation[3].

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

    VE-821 関連抗体
    分子量

    368.41

    分子式

    C18H16N4O3S
    CAS 番号
    Appearance

    Solid

    Color

    Light green to green

    SMILES

    O=C(NC1=CC=CC=C1)C2=NC(C3=CC=C(C=C3)S(=O)(C)=O)=CN=C2N
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 50 mg/mL (135.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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    • Dilution Calculator

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

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    =
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    ×
    Volume
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    Molecular Weight *

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

    C2

    ×
    体積 （終了）

    V2

    体内:

    The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

    • Protocol 1

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

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

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    (per animal)

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    純度とドキュメンテーション
    参考文献
    キナーゼ実験
    [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].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    細胞実験
    [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].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 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
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    VE-821 Related Classifications

    • Molarity Calculator

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    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    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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    製品名:
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    製品番号:
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