1. Protein Tyrosine Kinase/RTK
  2. Src
  3. PP2

PP2  (Synonyms: AGL 1879)

目录号: HY-13805 纯度: 99.35%
COA 产品使用指南

PP2 是可逆,ATP 竞争性的 Src 家族抑制剂,抑制 LckFynIC50 分别为 4 和 5 nM。

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PP2 Chemical Structure

PP2 Chemical Structure

CAS No. : 172889-27-9

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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 ¥1026
In-stock
50 mg ¥2530
In-stock
100 mg ¥4189
In-stock
200 mg   询价  
500 mg   询价  

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Customer Review

MCE 顾客使用本产品发表的 40 篇科研文献

WB
IF

    PP2 purchased from MCE. Usage Cited in: FASEB J. 2020 Aug;34(8):10443-10461.  [Abstract]

    Cells are pretreated with PP2 (10 μM) for 24 hours and further treated with MMS, and GAPDH nuclear translocation is visualized by confocal microscopy. The immunofluorescence staining results directly show that inhibiting Src activity by PP2 decreases GAPDH nuclear distribution in response to MMS.

    PP2 purchased from MCE. Usage Cited in: Cancer Sci. 2018 May;109(5):1648-1659.  [Abstract]

    Cells are treated with vehicle (0.1% DMSO) or PP2 (2.5 μM and 5 μM) for 48 h. Cell lysates are harvested. Total and phosphorylated c-Src are detected by western blotting.

    PP2 purchased from MCE. Usage Cited in: J Cell Mol Med. 2018 May 12;22(8):3768-3781.  [Abstract]

    Prostate cancer cells are grown and treated with different concentrations of the Src inhibitor PP2 for 2 h and subjected to Western blot analysis. The data show that the inhibition of Src dose dependently decreases levels of p-Src527 but not p-Src426.

    PP2 purchased from MCE. Usage Cited in: Oncotarget. 2017 Nov 22;8(65):109135-109150.  [Abstract]

    MCF-7 cells are pretreated with the indicated chemical inhibitors for 30min, followed by 15 min treatment with RA (20 μM) + EPA (80 μM).Cell extracts are prepared and subjected to western blotting analysis.

    PP2 purchased from MCE. Usage Cited in: Zhonghua Wei Zhong Bing Ji Jiu Yi Xue. 2015 Jul;27(7):568-73.  [Abstract]

    To determine whether the inhibition of caveolin-1 tyrosine residues 14 ( Cav-1-Y14 ) phosphorylation with protein tyrosine kinase inhibitors ( PP2 ) will upregulate heme oxygenase-1 ( HO-1 ) activity to protect against ventilation induced lung injury in vivo of an animal model. The group D1 or D2 receive high tidal volume ventilation for 1 hour or 2 hour respectively, but they are given PP2 1 hour before high tidal volume ventilation. The groups E1 and E2 also receive high tidal volume ventilat

    查看 Src 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

    PP2 is a reversible and ATP-competitive Src family kinases inhibitor with IC50s of 4 and 5 nM for Lck and Fyn, respectively.

    IC50 & Target

    IC50: 4 nM (Lck), 5 nM (Fyn)[1]

    体外研究
    (In Vitro)

    At 10 μM, the effect of PP2 on cellular proliferation is not significant, indicating that, at this low concentration, the effect of PP2 on Gemcitabine cytotoxicity does not simply reflect a direct antiproliferative effect, but rather a potentiation of Gemcitabine-induced cytotoxicity. Above 20 μM, growth is increasingly suppressed, a finding consistent with reports in other human cancer cell lines. Although 10 μM PP2 is used in our study, at higher concentrations PP2 is reported to inhibit other intracellular kinases[2]. PP2 is the most widely used commercially available Src family kinase inhibitor. PP2 inhibits Src family kinase activity with IC50 of ~5 nM in vitro, concentrations to 10 μM are often necessary to achieve complete Src family kinase inhibition in cell culture[3].

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

    体内研究
    (In Vivo)

    The tumor growth inhibition rate is 25% in the PP2 treatment group and 5% in the Gemcitabine treatment group (P>0.05). When administered in combination, PP2 and Gemcitabine produce a tumor growth inhibition rate of 98% (P<0.05). Hepatic metastasis occurred in 100% of control and Gemcitabine-treated groups; 88% of the PP2-treated group developed liver metastases. There are no detectable metastases in the group treated with PP2 and Gemcitabine in combination (P<0.05)[2].

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

    分子量

    301.77

    Formula

    C15H16ClN5

    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 1 year
    -20°C 6 months
    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : 50 mg/mL (165.69 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)

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

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 3.3138 mL 16.5689 mL 33.1378 mL
    5 mM 0.6628 mL 3.3138 mL 6.6276 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: ≥ 3 mg/mL (9.94 mM); 澄清溶液

      此方案可获得 ≥ 3 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 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    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
    参考文献
    Cell Assay
    [2]

    Cell growth is determined by MTT assay and confirmed by cell counting. Results of the MTT assay have been shown to correlate well with [3H]thymidine incorporation in pancreatic cancer cell lines. Logarithmically growing cells are plated at 5×103 cells/well in 96-well plates, allowed to adhere for 24 h, and cultured in the presence or absence of PP2 and Gemcitabine. Cell proliferation is determined after 96 h. Plates are read using a Vmax microplate spectrophotometer at a wavelength of 570 nm corrected to 650 nm and normalized to controls. Each independent experiment is performed three times, with 10 determinations for each condition tested. The IC50 of Gemcitabine is calculated from these results. At identical time points, cells are trypsinized to form a single cell suspension. Intact cells, determined by trypan blue exclusion, are counted using a Neubauer hemocytometer, and the number of cells per mL is calculated and compared with the control group to confirm the MTT results[2].

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

    Animal Administration
    [2]

    Mice[2]
    Male athymic nu/nu mice (age, 5 weeks; weight, 20-22 g; specific pathogen free) are anesthetized with i.p. ketamine (200 mg/kg) and xylazine (10 mg/kg) and inoculated with 106 Gemcitabine-resistant PANC1GemRes cells in 20 μL of PBS by surgical orthotopic implantation into the pancreas. After inoculation, mice are randomized to three treatment groups: (a) treatment group 1 (n=8) receive 2 mg/kg PP2 in 1% DMSO by i.p. injection three times a week; (b) treatment group 2 (n=8) receive Gemcitabine (100 mg/kg) in the same volume of 1% DMSO vehicle as received by group 1, three times a week; and (c) treatment group 3 (n=8) receive 2 mg/kg PP2 and 100 mg/kg Gemcitabine in the same volume of DMSO as groups 1 and 2, three times a week. The control group receive the same volume of 1% DMSO vehicle as the other groups, three times a week. Treatment is commenced 1 day after implantation, and necropsy is performed 4 weeks after implantation. Primary tumors are identified, weighed, and normalized to total body mass. Tumor growth inhibition rate is calculated using the following formula: tumor growth inhibition rate (%)=(1−MT/MC)×100, where MT and MC are the mean normalized tumor masses of treatment and control groups, respectively. Liver metastases are counted and confirmed histologically.

    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 3.3138 mL 16.5689 mL 33.1378 mL 82.8446 mL
    5 mM 0.6628 mL 3.3138 mL 6.6276 mL 16.5689 mL
    10 mM 0.3314 mL 1.6569 mL 3.3138 mL 8.2845 mL
    15 mM 0.2209 mL 1.1046 mL 2.2092 mL 5.5230 mL
    20 mM 0.1657 mL 0.8284 mL 1.6569 mL 4.1422 mL
    25 mM 0.1326 mL 0.6628 mL 1.3255 mL 3.3138 mL
    30 mM 0.1105 mL 0.5523 mL 1.1046 mL 2.7615 mL
    40 mM 0.0828 mL 0.4142 mL 0.8284 mL 2.0711 mL
    50 mM 0.0663 mL 0.3314 mL 0.6628 mL 1.6569 mL
    60 mM 0.0552 mL 0.2761 mL 0.5523 mL 1.3807 mL
    80 mM 0.0414 mL 0.2071 mL 0.4142 mL 1.0356 mL
    100 mM 0.0331 mL 0.1657 mL 0.3314 mL 0.8284 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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    目录号:
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