2. Cell Cycle/DNA Damage PI3K/Akt/mTOR
  3. ATM/ATR
  4. AZ20

AZ20 是一种有效的，选择性的 ATR 抑制剂，IC50 值为 5 nM；同时可抑制 mTOR 活性，IC50 值为 38 nM。

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AZ20 Chemical Structure

AZ20 Chemical Structure

CAS No. : 1233339-22-4

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥660
In-stock
1 mg ￥272
In-stock
5 mg ￥600
In-stock
10 mg ￥900
In-stock
50 mg ￥2900
In-stock
100 mg ￥4500
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

AZ20 相关抗体

Top Publications Citing Use of Products

    AZ20 purchased from MCE. Usage Cited in: Cell Death Dis. 2017 Aug 10;8(8):e2982.  [Abstract]

    Tumor pieces from M130116 PDXs treated with the vehicle or the RVX2135/AZ20 combination treatment are subjected to western blot analysis.

    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

    AZ20 is a potent and selective inhibitor of ATR with an IC50 of 5 nM, and has 8-fold selectivity against mTOR (IC50=38 nM).

    IC50 & Target[1]

    ATR

    5 nM (IC50)

    mTOR

    38 nM (IC50)

    PI3Kα

    13000 nM (IC50)

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    0.7 μM
    Compound: AZ20
    Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay
    Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay
    		[PMID: 35191694]
    HeLa IC50
    0.005 μM
    Compound: 6, AZ20
    Inhibition of ATR in human HeLa cell nuclear extracts using glutathione S-transferase-p53N66 and ATP as substrate incubated for 10 mins prior to ATP addition measured after 1 hr by ELISA
    Inhibition of ATR in human HeLa cell nuclear extracts using glutathione S-transferase-p53N66 and ATP as substrate incubated for 10 mins prior to ATP addition measured after 1 hr by ELISA
    		[PMID: 23394205]
    HT-29 IC50
    0.05 μM
    Compound: 6, AZ20
    Inhibition of ATR-mediated CHK1 phosphorylation at serine 345 in human HT29 cells after 1 hr in presence of 4-nitroquinoline 1-oxide
    Inhibition of ATR-mediated CHK1 phosphorylation at serine 345 in human HT29 cells after 1 hr in presence of 4-nitroquinoline 1-oxide
    		[PMID: 23394205]
    HT-29 GI50
    0.97 μM
    Compound: 1; AZ20
    Cytotoxicity against human HT-29 cells after 72 hrs by MTS assay
    Cytotoxicity against human HT-29 cells after 72 hrs by MTS assay
    		[PMID: 30346772]
    LoVo GI50
    0.2 μM
    Compound: 1; AZ20
    Cytotoxicity against human LoVo cells after 72 hrs by MTS assay
    Cytotoxicity against human LoVo cells after 72 hrs by MTS assay
    		[PMID: 30346772]
    LoVo GI50
    0.2 μM
    Compound: 6, AZ20
    Growth inhibition of human LoVo cells after 72 hrs by MTS assay
    Growth inhibition of human LoVo cells after 72 hrs by MTS assay
    		[PMID: 23394205]
    体外研究
    (In Vitro)

    AZ20 抑制 HeLa 核提取物中免疫沉淀的 ATR，IC50 为 5 nM，ATR 介导的 Chk1 磷酸化在 HT29 结直肠腺癌肿瘤细胞中的 IC50 为 50 nM[1]。

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

    AZ20 相关抗体:
    体内研究
    (In Vivo)

    AZ20 (25、50 mg/kg，口服) 具有高渗透性和对大鼠肝细胞的良好稳定性，尽管在实现显著更高的溶解度方面缺乏进展，但在低剂量大鼠 PK 研究中具有可观的生物利用度。AZ20 (25，50 mg/kg，po) 对携带 LoVo 肿瘤的雌性裸鼠显著抑制肿瘤生长[1]。

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

    412.51

    Formula

    C21H24N4O3S
    CAS 号
    性状

    固体

    颜色

    White to off-white

    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 2 years
    -20°C 1 year
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : ≥ 100 mg/mL (242.42 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.4242 mL 12.1209 mL 24.2418 mL
    5 mM 0.4848 mL 2.4242 mL 4.8484 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 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：

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.06 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.06 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
    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
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.40%

    COA (296 KB) LCMS (102 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [1]

    Compound dose ranges are created by diluting in 100% DMSO and then further into assay medium (EMEM, 10% FCS, 1% glutamine) using a Labcyte Echo acoustic dispensing instrument. Cells are plated in 384-well Costar plates at 9×104 cells per mL in 40 μL of EMEM, 10% FCS, 1% glutamine and grown for 24 h. Following addition of compound the cells are incubated for 60 min. A final concentration of 3 μM 4NQO (prepared in 100% DMSO) is then added using the Labcyte Echo, and the cells are incubated for a further 60 min. The cells are fixed by adding 40 μL of 3.7% v/v formaldehyde solution for 20 min. After removal of fix, cells are washed with PBS and permeabilized in 40 μL of PBS containing 0.1% Triton X-100. The cells are then washed, and 15 μL primary antibody solution (pChk1 Ser345) is added. The plates are incubated at 4°C overnight. The primary antibody is then washed off, and 20 μL of secondary antibody solution and 1 μM Hoechst 33258 added for 90 min at room temperature. The plates are washed and left in 40 μL of PBS. Plates are then read on an ArrayScan VTI instrument to determine staining intensities, and dose responses are obtained and used to determine the IC50 values for the compounds.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Female Swiss nu/nu mice are housed in negative pressure isolators. LoVo tumor xenografts are established in 8- to 12-week-old mice by injecting 1×107 tumor cells subcutaneously (100 μL in serum free medium) on the left dorsal flank. Animals are randomized into treatment groups when tumors become palpable. AZ20 is prepared in 10% DMSO/40% propylene glycol/50% water and administered orally. Tumors are measured up to three times per week with calipers. Tumor volumes are calculated and the data plotted using the geometric mean for each group versus time.

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

    AZ20 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.4242 mL 12.1209 mL 24.2418 mL 60.6046 mL
    5 mM 0.4848 mL 2.4242 mL 4.8484 mL 12.1209 mL
    10 mM 0.2424 mL 1.2121 mL 2.4242 mL 6.0605 mL
    15 mM 0.1616 mL 0.8081 mL 1.6161 mL 4.0403 mL
    20 mM 0.1212 mL 0.6060 mL 1.2121 mL 3.0302 mL
    25 mM 0.0970 mL 0.4848 mL 0.9697 mL 2.4242 mL
    30 mM 0.0808 mL 0.4040 mL 0.8081 mL 2.0202 mL
    40 mM 0.0606 mL 0.3030 mL 0.6060 mL 1.5151 mL
    50 mM 0.0485 mL 0.2424 mL 0.4848 mL 1.2121 mL
    60 mM 0.0404 mL 0.2020 mL 0.4040 mL 1.0101 mL
    80 mM 0.0303 mL 0.1515 mL 0.3030 mL 0.7576 mL
    100 mM 0.0242 mL 0.1212 mL 0.2424 mL 0.6060 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:

    AZ201233339-22-4AZ 20AZ-20ATM/ATRAtaxia telangiectasia mutatedATM and RAD3 relatedInhibitorinhibitorinhibit

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