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  3. AEE788

AEE788  (Synonyms: NVP-AEE 788)

目录号: HY-10045 纯度: 99.13%
COA 产品使用指南

AEE788是EGFRErbB2的抑制剂,IC50值分别为2和6 nM。

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AEE788 Chemical Structure

AEE788 Chemical Structure

CAS No. : 497839-62-0

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规格 价格 是否有货 数量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ¥880
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5 mg ¥800
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10 mg ¥1300
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50 mg ¥4200
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100 mg ¥6700
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500 mg   询价  

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Top Publications Citing Use of Products

    AEE788 purchased from MCE. Usage Cited in: Oncol Rep. 2018 Nov;40(5):2944-2954.  [Abstract]

    The EGFR/PI3K/AKT signaling pathway is significantly suppressed in A549 cells treated with AEE788 (0.5 nM, 48 h) following miR-145 upregulation, compared with the miR-145 upregulation group.

    AEE788 purchased from MCE. Usage Cited in: Int J Clin Exp Med. 2016;9(8):15892-15899.

    The protein expressions of EGFR are detected by Western blot in CNE1 after 5 nM AEE788 treatment for 4 hs, compared with the control.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    AEE788 is an inhibitor of the EGFR and ErbB2 with IC50 values of 2 and 6 nM, respectively.

    IC50 & Target[1]

    EGFR

    2 nM (IC50)

    ErbB2

    6 nM (IC50)

    体外研究
    (In Vitro)

    AEE788 在纳摩尔范围内抑制 EGFRVEGF 受体酪氨酸激酶 (IC50:EGFR 2 nm、ErbB2 6 nm、KDR 77 nm 和 Flt-1 59 nm)。在细胞中,生长因子诱导的 EGFR 和 ErbB2 磷酸化也被有效抑制 (IC50 分别为 11 和 220 nm)。AEE788 对一系列 EGFR 和 ErbB2 过表达细胞系 (包括 EGFRvIII 依赖性细胞系) 具有抗增殖活性,并抑制表皮生长因子和 VEGF 刺激的人脐静脉内皮细胞的增殖[1]。AEE788 处理皮肤 SCC 细胞导致 EGFR 和 VEGFR-2 磷酸化的剂量依赖性抑制、生长抑制并诱导细胞凋亡[2]

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

    体内研究
    (In Vivo)

    AEE788 有效抑制肿瘤中生长因子诱导的 EGFR 和 ErbB2 磷酸化,该抑制活性超过 72 小时。AEE788 还在小鼠植入模型中抑制 VEGF 诱导的血管生成[1]。AEE788 在治疗开始后 21 天,抑制了 54% 的肿瘤生长[2]

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

    Clinical Trial
    分子量

    440.58

    Formula

    C27H32N6

    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
    In Vitro: 

    DMSO 中的溶解度 : 50 mg/mL (113.49 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 2.2697 mL 11.3487 mL 22.6974 mL
    5 mM 0.4539 mL 2.2697 mL 4.5395 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

    In Vivo:

    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 (5.67 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。
    • 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 (5.67 mM); 悬浊液; 超声助溶

      此方案可获得 2.5 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      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。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):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

    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: 99.13%

    参考文献
    Kinase Assay
    [1]

    The invitro kinase assays are performed in 96-well plates (30 μL) at ambient temperature for 15–45 min using the recombinant glutathione S-transferase-fused kinase domains (4–100 ng, depending on specific activity). [γ33P]ATP is used as phosphate donor and polyGluTyr-(4:1) peptide as acceptor. Assays are optimized for each kinase using the following ATP concentrations: 1.0 μM (c-Kit, c-Met, c-Fms, c-Raf-1, and RET), 2.0 μM (EGFR, ErbB2, ErbB3, and ErbB4), 5.0 μM (c-Abl), 8.0 μM (Flt-1, Flt-3, Flt-4, Flk, KDR, FGFR-1, and Tek), 10.0 μM (PDGF receptor-β, protein kinase C-α, and cyclin-dependent kinase 1), and 20.0 μM (c-Src and protein kinase A). The reaction is terminated by the addition of 20 μL 125 mM EDTA. Thirty μL (c-Abl, c-Src, insulin-like growth factor-1R, RET-Men2A, and RET-Men2B) or 40 μL (all other kinases) of the reaction mixture is transferred onto Immobilon-polyvinylidene difluoride membrane, presoaked with 0.5% H3PO4 and mounted on a vacuum manifold. Vacuum is then applied and each well rinsed with 200 μL 0.5% H3PO4. Membranes are removed and washed four times. Dried membranes are counted. IC50 are calculated by linear regression analysis of the percentage inhibition and are averages of at least three determinations[1].

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

    Cell Assay
    [2]

    AEE788 is dissolved in 90% polyethylene glycol 300 plus 10% 1-methyl-2-pyrrolidinone to a concentration of 6.25 mg/mL. Tumor cells are seeded into 96-well plates in complete medium and allowed to attach for 24 hours. The cultures are re-fed with medium with 2% serum. After 24 hours, cells are treated with different concentrations (0-2 μM) of AEE788 (negative control with DMSO alone) for 72 hours. After a 2-hour incubation in medium containing 0.42 mg/mL MTT, the cells are lysed in 100 μL DMSO. The conversion of MTT to formazan is measured at an absorbance of 570 nm[2]

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

    Animal Administration
    [1]

    Mice: AEE788 is diluted in DMSO and diluted in the optimal medium. BALB/c mice bearing s.c. A-431 squamous tumors (3 animals/group) or HC11-NeuT-driven breast tumors (2 animals/group) are dosed orally with 30 mg/kg of AEE788 or vehicle once daily for 5 days. At different time points after the end of compound treatment and before sacrificing the animals the mice are given i.v. 500 μg EGF/kg body weight or 0.2 ml 0.9% w/v NaCl as vehicle control. Five min after EGF administration, the mice are sacrificed, tumors are removed[1].

    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, 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 2.2697 mL 11.3487 mL 22.6974 mL 56.7434 mL
    5 mM 0.4539 mL 2.2697 mL 4.5395 mL 11.3487 mL
    10 mM 0.2270 mL 1.1349 mL 2.2697 mL 5.6743 mL
    15 mM 0.1513 mL 0.7566 mL 1.5132 mL 3.7829 mL
    20 mM 0.1135 mL 0.5674 mL 1.1349 mL 2.8372 mL
    25 mM 0.0908 mL 0.4539 mL 0.9079 mL 2.2697 mL
    30 mM 0.0757 mL 0.3783 mL 0.7566 mL 1.8914 mL
    40 mM 0.0567 mL 0.2837 mL 0.5674 mL 1.4186 mL
    50 mM 0.0454 mL 0.2270 mL 0.4539 mL 1.1349 mL
    60 mM 0.0378 mL 0.1891 mL 0.3783 mL 0.9457 mL
    80 mM 0.0284 mL 0.1419 mL 0.2837 mL 0.7093 mL
    100 mM 0.0227 mL 0.1135 mL 0.2270 mL 0.5674 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:
    AEE788
    目录号:
    HY-10045
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