1. PI3K/Akt/mTOR Autophagy Apoptosis
  2. mTOR Autophagy Apoptosis
  3. AZD-8055

AZD-8055 是一种有效、选择性、具有口服活性和 ATP 竞争性的 mTOR 抑制剂,IC50 为 0.8 nM。AZD-8055 抑制 mTORC1mTORC2

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AZD-8055 Chemical Structure

AZD-8055 Chemical Structure

CAS No. : 1009298-09-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥506
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5 mg ¥460
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10 mg ¥750
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50 mg ¥1880
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100 mg ¥2980
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200 mg ¥4850
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Customer Review

MCE 顾客使用本产品发表的 45 篇科研文献

WB

    AZD-8055 purchased from MCE. Usage Cited in: Heliyon. 2023 Mar 6.

    AZD8055 (100, 500, 1000 nM; 48h) significantly suppresses the expression of pAKT, p-S6K1 and p-mTOR in both the T24 and 5637 human bladder urothelial carcinoma cell lines, and the SCaBER and UM-UC-3 human bladder squamous cell carcinoma cell line.

    AZD-8055 purchased from MCE. Usage Cited in: Cancer Sci. 2018 Jan;109(1):103-111.  [Abstract]

    ATL-43T cell lines are treated for 0 and 60 min with control (DMSO), Rapamycin, RAD001, LY294002, PP242 and AZD8055. After treatment, protein lysates are immunoblotted for expression of phosphorylated mTOR S2448 (mTORC1), S2481 (mTORC2), total mTOR, p-Akt S473, total Akt, p-p70S6k, total p70S6k, and actin.

    AZD-8055 purchased from MCE. Usage Cited in: Cancer Sci. 2018 Jan;109(1):103-111.  [Abstract]

    HUT-102 cell lines are treated for 0 and 60 min with control (DMSO), Rapamycin, RAD001, LY294002, PP242 and AZD8055. After treatment, protein lysates are immunoblotted for expression of phosphorylated mTOR S2448 (mTORC1), S2481 (mTORC2), total mTOR, p-Akt S473, total Akt, p-p70S6k, total p70S6k, and actin.

    AZD-8055 purchased from MCE. Usage Cited in: Cancer Sci. 2018 Jan;109(1):103-111.  [Abstract]

    ED-40415 cell lines are treated for 0 and 60 min with control (DMSO), Rapamycin, RAD001, LY294002, PP242 and AZD8055. After treatment, protein lysates are immunoblotted for expression of phosphorylated mTOR S2448 (mTORC1), S2481 (mTORC2), total mTOR, p-Akt S473, total Akt, p-p70S6k, total p70S6k, and actin.

    AZD-8055 purchased from MCE. Usage Cited in: Cancer Sci. 2018 Jan;109(1):103-111.  [Abstract]

    MT-2 cell lines are treated for 0 and 60 min with control (DMSO), Rapamycin, RAD001, LY294002, PP242 and AZD8055. After treatment, protein lysates are immunoblotted for expression of phosphorylated mTOR S2448 (mTORC1), S2481 (mTORC2), total mTOR, p-Akt S473, total Akt, p-p70S6k, total p70S6k, and actin.

    AZD-8055 purchased from MCE. Usage Cited in: Oncotarget. 2017 Jul 11;8(28):45793-45806.  [Abstract]

    Cells are treated for 2 h with AZD8055 at the indicated concentrations (0, 50, 200 and 800 nM), and cell lysates are probed with phosphor- and total antibodies of mTOR signaling pathway. β-actin is used as loading control. Blot shown is representative of at least two independent experiments.

    AZD-8055 purchased from MCE. Usage Cited in: Oncotarget. 2017 Feb 21;8(8):12775-12783.  [Abstract]

    OSI-027, AZD-8055 and AZD-2014 almost completely block MHY1485-induced mTOR activation (p-mTOR/S6K1/Akt Ser473) in skin keratinocytes.

    AZD-8055 purchased from MCE. Usage Cited in: PLoS One. 2016 Jan 28;11(1):e0147682.  [Abstract]

    CHP-212 and SK-N-AS cells are treated with indicated concentrations of AZD6244, MEK162, RAD001 or AZD8055 or combinations thereof as indicated for 1 hour. Then, cells are lysed and analysed by Western blot. Phosphorylation levels of AKT, ERK and S6 are detected by specific anti-phospho antibodies. Loading is verified by specific antibodies to total AKT, ERK and anti-tubulin.

    AZD-8055 purchased from MCE. Usage Cited in: Sci Bull. 2015 Dec;60(24):2120-2128.

    CNE-2Z cells are treated with AZD8055 or Rapamycin with or without 1 T SMF for 3 d before they are harvested for Western blot.

    AZD-8055 purchased from MCE. Usage Cited in: Oncotarget. 2015 Dec 8;6(39):42183-96.  [Abstract]

    KNS-62 and T24 cells are treated with 250 nM AZD6244, 250 nM MEK162, 5 nM of RAD001, 250 nM AKT8055 or combinations thereof as indicated for 1 hour. Then, cells are lysed and analysed by Western blot.

    AZD-8055 purchased from MCE. Usage Cited in: Cancer Res. 2013 Apr 15;73(8):2574-86.  [Abstract]

    Cells are treated with the indicated concentrations of AZD8055, Torin2 or staurosporin overnight and analyzed by western blot using antibodies specific for the indicated proteins.

    查看 mTOR 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    AZD-8055 is a potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8 nM. AZD-8055 inhibits both mTORC1 and mTORC2[1].

    IC50 & Target

    mTOR

    0.8 nM (IC50)

    mTORC1

     

    mTORC2

     

    Autophagy

     

    体外研究
    (In Vitro)

    The inhibitory activity of AZD-8055 (AZD8055) against mTOR is evaluated using two different assays. Using the truncated recombinant mTOR enzyme, the IC50 for AZD8055 is 0.13±0.05 nM. Using native mTOR enzyme complexes extracted from HeLa cells, the IC50 is 0.8±0.2 nM. AZD-8055 shows excellent selectivity (~1,000-fold) against all class I PI3K isoforms and other members of the PI3K-like kinase family. AZD-8055 inhibits the phosphorylation of mTORC1 substrates p70S6K and 4E-BP1 as well as phosphorylation of the mTORC2 substrate AKT and downstream proteins. The cellular IC50s for AZD8055 are calculated as 24±9 nM (n=13) for pAKT Ser473 and 27±3 nM (n=12) for pS6 Ser235/236 in MDA-MB-468 cells[1].

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

    体内研究
    (In Vivo)

    In mice bearing U87-MG (PTEN null) glioblastoma xenografts, oral treatment with AZD-8055 (AZD8055) results in a dose-dependent tumor growth inhibition of 33%, 48%, and 77% with 2.5, 5, and 10 mg/kg/d twice daily, respectively. A similar dose dependency is observed in nude mice bearing A549 xenografts: tumor growth inhibition is 44%, 55%, and 93% after 2.5, 5, and 10 mg/kg/d twice daily, respectively. AZD8055 also results in significant inhibition of tumor growth and/or regression in breast, lung, colon, prostate, and uterine xenograft models when administered either twice daily at 10 mg/kg or daily at a dose of 20 mg/kg[1]. AZD8055 markedly decreases the phosphorylation levels of mTOR and its substrates and the activation of microglia in vivo, and promotes the microglial polarization from M1 phenotype to M2 phenotype. In addition, administration of AZD8055 following subarachnoid hemorrhage (SAH) significantly ameliorates EBI, including neuronal apoptosis, neuronal necrosis, brain edema and blood-brain barrier permeability[2].

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

    Clinical Trial
    分子量

    465.54

    Formula

    C25H31N5O4

    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    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 : 33.33 mg/mL (71.59 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)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.1480 mL 10.7402 mL 21.4804 mL
    5 mM 0.4296 mL 2.1480 mL 4.2961 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:

    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    90% Corn Oil

      Solubility: ≥ 5 mg/mL (10.74 mM); 澄清溶液

      此方案可获得 ≥ 5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

      1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    • 方案 二

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

      Solubility: ≥ 2.5 mg/mL (5.37 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。

      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。

    以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 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: 30% SBE-β-CD in Saline

      Solubility: 50 mg/mL (107.40 mM); 澄清溶液; 超声助溶; 酸性条件溶解 (HCL 调节,pH≈2)

    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

    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: 99.60%

    参考文献
    Kinase Assay
    [1]

    Inhibition of mTOR is evaluated using two methodologies: The high-throughput assay uses an α screen capture complex technology with a recombinant truncated FLAG-tagged mTOR (amino acids 1362-2549; expressed in HEK293 cells) and a biotinylated p70 peptide substrate. In addition, native mTOR activity is assayed using immunoprecipitation of full-length mTOR from HeLa cytoplasmic extract, and the endogenous mTOR is in protein complexes with Rictor and Raptor. A kinase assay is performed in the presence of recombinant 4E-BP1 protein as substrate with detection of the phosphorylated product through an ELISA format. The activity of the lipid kinases, class I PI3Ks α, β, δ, and γ, is measured using recombinant PI3Ks with the lipid PIP2 as substrate. Assays for the ataxia-telangiectasia mutated (ATM) and DNA-PK are performed. Finally, counterscreen against 260 kinases is carried out at a fixed concentration of 10 μM AZD-8055[1].

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

    Cell Assay
    [1]

    For growth inhibition and acridine staining, cells are exposed to increasing concentrations of AZD-8055 (0 to 1,280 nM) for 72 to 96 h and stained for cell nuclei (0.03 mg/mL Hoechst 33342) and acidic vesicles (1 μg/mL acridine orange). Images are captured at 450 and 536 nm on an ArrayScan II platform, and the percentage of acidic vesicles and the number of cells are quantified. For LC3 assessment, cells are exposed to e64d/pepstatin (10 μg/mL) for 30 to 90 min before incubation with AZD8055. Cells are lysed on ice and analyzed by immunoblotting[1].

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

    Animal Administration
    [1][2]

    Mice[1]
    Tumor cells (106 for U87-MG, 5×106 for A549) are injected s.c. in a volume of 0.1 mL, and mice are randomized into control and treatment groups when tumor size reach 0.2 cm3. AZD-8055 is administered by oral gavage (0.1 mL/10 g of body weight) once or twice daily. The control group receive the vehicle only. Tumor volumes (measured by caliper), animal body weight, and tumor condition are recorded twice weekly for the duration of the study. The tumor volume is calculated.
    Rats[2]
    Sprague-Dawley (SD) rats (250 g) and pregnant SD rats (16-18 days gestation, used for microglia extraction) are used. In experiment 1, 48 rats (54 rats are used, 48 rats survive after the surgery) are assigned randomly to four groups: sham group, SAH 3 h group, SAH 24 h group, SAH 72 h group. The animals in SAH 3 h, 24 h and 72 h groups are subjected to experimental SAH and are killed at 3 h, 24 h and 72 h after blood injection, respectively (n=12 for each group). In experiment 2, 72 rats (83 rats are used, 72 rats survive after the surgery) are assigned randomly to sham group (n=18), SAH+vehicle group (n=18), SAH+Rapamycin group (n=18), SAH+AZD8055 group (n=18). The rat receive a single intraperitoneal injection of Rapamycin immediately after induction of SAH, the dose of Rapamycin used is 150 μg/kg body weight. AZD8055 is administered by oral gavage with the dose of 14 mg/kg body weight. Rats in vehicle group are treated with equal volume solvent. All the rats in experiment 2 are killed at 24 h post-SAH. In experiment 3, enriched microglia are distributed into 5 groups: Control, OxyHb, OxyHb+vehicle (DMSO), OxyHb+Rapamycin and OxyHb+AZD8055. Twenty-four hours after microglia re-seeding, cells are treated with OxyHb (10 μM), DMSO (volume equal to Rapamycin and AZD8055), Rapamycin (2.74 mM), AZD8055 (0.8 nM) respectively in fresh medium. After incubation for 24 h (in 37°C, 5% CO2), cell medium is removed, washed by PBS for 3 times and fixed by 4% paraformaldehyde.

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

    参考文献

    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 2.1480 mL 10.7402 mL 21.4804 mL 53.7011 mL
    5 mM 0.4296 mL 2.1480 mL 4.2961 mL 10.7402 mL
    10 mM 0.2148 mL 1.0740 mL 2.1480 mL 5.3701 mL
    15 mM 0.1432 mL 0.7160 mL 1.4320 mL 3.5801 mL
    20 mM 0.1074 mL 0.5370 mL 1.0740 mL 2.6851 mL
    25 mM 0.0859 mL 0.4296 mL 0.8592 mL 2.1480 mL
    30 mM 0.0716 mL 0.3580 mL 0.7160 mL 1.7900 mL
    40 mM 0.0537 mL 0.2685 mL 0.5370 mL 1.3425 mL
    50 mM 0.0430 mL 0.2148 mL 0.4296 mL 1.0740 mL
    60 mM 0.0358 mL 0.1790 mL 0.3580 mL 0.8950 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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    产品名称:
    AZD-8055
    目录号:
    HY-10422
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