1. PI3K/Akt/mTOR Apoptosis
  2. mTOR Apoptosis
  3. Palomid 529

Palomid 529  (Synonyms: P529)

目录号: HY-14581 纯度: 99.47%
COA 产品使用指南

Palomid 529 是一种有效的 mTORC1mTORC2 复合体抑制剂。

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Palomid 529 Chemical Structure

Palomid 529 Chemical Structure

CAS No. : 914913-88-5

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Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ¥550
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5 mg ¥500
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10 mg ¥800
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50 mg ¥2500
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100 mg ¥3750
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500 mg   询价  

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Top Publications Citing Use of Products

    Palomid 529 purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Mar 4;497(2):499-505.  [Abstract]

    mTOR signaling in RES-529-treated or vehicle–treated tumor tissues is analyzed by a Western blotting assay.

    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

    Palomid 529 is a potent inhibitor of mTORC1 and mTORC2 complexes.

    IC50 & Target[1]

    TORC1

     

    TORC2

     

    体外研究
    (In Vitro)

    Palomid 529 (P529) inhibits both VEGF-driven (IC50, 20 nM) and bFGF-driven (IC50, 30 nM) endothelial cell proliferation and retained the ability to induce endothelial cell apoptosis[1]. Palomid 529 (RES-529) is a PI3K/AKT/mTOR pathway inhibitor that interferes with the pathway through both mTOR complex 1 (mTORC1) and mTOR complex 2 (mTORC2) dissociation. Palomid 529 inhibits mTORC1/mTORC2 activity in various cancer cell lines, as noted by decreased phosphorylation of substrates including ribosomal protein S6, 4E-BP1, and AKT, leading to cell growth inhibition and death, with activity generally in the range of 5-15 μM. At 10 μM concentrations, Palomid 529 reduces the binding of 0.5 nM [3H]estradiol to estrogen receptor (ER)α and ERβ by 3% or less. Palomid 529 inhibits both VEGF-stimulated and β fibroblast growth factor-stimulated HUVEC cell proliferation with IC50 of ~10 and 30 nM, respectively. Treatment of HUVEC cells with Palomid 529 also results in a four-fold induction of apoptosis on the basis of DNA fragmentation. Growth inhibition is observed with Palomid 529 treatment in various cancer cell lines from the National Cancer Institute-60 (NCI-60) tumor panel, with IC50 ranges of 5-15 μM for central nervous system cancer cells and 5-30 μM for prostate cancer cells[2]. Palomid 529 (P529) results in a dose- and time-dependent decrease in Akt activity in PC3, LnCaP, and 22rv1 cells as evidenced by a reduced phosphorylation of Akt (Ser473). Similar results are observed in all PCa cells with similar enzymatic IC50s of about 0.2 μM. Palomid 529 inhibits the cell proliferation of neoplastic cells at different extent (IC50s ranged from 5 to 28 μM), whereas very few effects are observed in non-neoplastic BPH1 and EPN cells. Treatment with Palomid 529 results in a concentration-dependent reduction in viable/proliferating tumor cells compared with non-neoplastic BPH1 and EPN cells. IC50s range from 5 to 28 μM[3].

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

    体内研究
    (In Vivo)

    Palomid 529 (200 mg/kg/2d) inhibits C6V10 glioma tumor growth in nude mice following i.p. dosing. Analysis of signaling within the tumor lysates reveals that Palomid 529 (P529) also reduces AktS473 but not AktT308 signaling[1]. Palomid 529 (RES-529) has shown antitumor activity in a variety of mouse models, including those for glioblastoma, and prostate and breast cancer. In a C6V10 glioblastoma subcutaneous xenograft model, mice pretreated with Palomid 529 (200 mg/kg/2 days, intraperitoneal) 1 week before and for 3 weeks after a tumor cell injection showed an ~70% decrease in tumor volume compared with the control. In another glioblastoma tumor model using human U87 cells, mice treated with micronized Palomid 529 3 days after a tumor cell injection showed a reduction in tumor growth by ~78 and 29% with 50 and 25 mg/kg/2 days, intraperitoneal, Palomid 529, respectively, after 24 days compared with the control[2]. Palomid 529 (P529) is able to reduce tumor growth in a dose-dependent manner both in PC3 and 22rv1 xenografts. A 10, 47.6, and 59.3% reduction of tumor mass is demonstrated in mice bearing PC3 xenografts receiving 50, 100, and 200 mg/kg Palomid 529 respectively and a 9, 38.7, and 51.5% reduction of tumor mass in mice bearing 22rv1 xenografts receiving 50, 100, and 200 mg/kg Palomid 529 respectively[3].

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

    Clinical Trial
    分子量

    406.43

    Formula

    C24H22O6

    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 : 100 mg/mL (246.04 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 2.4604 mL 12.3022 mL 24.6045 mL
    5 mM 0.4921 mL 2.4604 mL 4.9209 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    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (6.15 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,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 25.0 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

    纯度: 99.47%

    参考文献
    Kinase Assay
    [1]

    The proteins are produced with rabbit reticulocyte lysates that couples transcription and translation in a single reaction. The amount of template used in each reaction is determined empirically and expression is monitored in parallel reactions where [35S]methionine is incorporated into the receptor followed by gel electrophoresis and exposure to film. Binding reactions of the estrogen receptors (ER) and Palomid 529 (P529) are carried out in 100 mL final volumes in TEG buffer [10 mM Tris (pH 7.5), 1.5 mM EDTA, 10% glycerol]. In vitro transcribed-translated receptor (5 AL) is used in each binding reaction in the presence of 0.5 nM [3H]estradiol (E2). All compounds are routinely tested from 10−11 to 10−6 M and diluted in ethanol. The reactions are incubated at 4°C overnight and bound E2 is quantified by adding 200 mL dextran-coated charcoal. After a 15-min rotation at 4°C, the tubes are centrifuged for 10 min and 150 mL of the supernatant are added to 5 mL scintillation mixture for determination of cpm by liquid scintillation counting. The maximum binding is determined by competing bound E2 with only the ethanol vehicle. Controls for background are included in each experiment using 5 mL unprogrammed rabbit reticulocyte lysate. This value, typically 10% to 15% of the maximal counts, is subtracted from all values. The data are plotted and Kis are calculated using the Prism software. Experiments are conducted at least thrice in duplicate[1].

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

    Cell Assay
    [1]

    The proliferation assay is carried out by seeding the HUVECs in 96-well plates at a density of 1,000 per well in complete medium. Following a 24-h plating period, the cells are starved for 24 h in 0.5% serum before being treated with Palomid 529 in the presence of 10 ng/mL basic fibroblast growth factor (bFGF) or VEGF in complete medium. After 48 h, cell number is determined using a colorimetric method as described by the supplier. The results are expressed as the percentage of the maximal bFGF or VEGF response in the absence of P529. Nonproliferating endothelial cells are assayed by growing HUVECs to quiescence in 96-well plates and treating with Palomid 529 (0, 100, 200, 300 and 400 nM) for 48 h. Initially, 5,000 cells per well are seeded and confluence is achieved the next day. The plates are incubated for another 24 h to ensure growth arrest before treatment with P529. Cell number is determined as outlined above[1].

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

    Animal Administration
    [1]

    Mice[1]
    Four- to 6-wk-old female nude mice are pretreated with Palomid 529 (200 mg/kg/2d, i.p.) for 1 wk, and then 1×105 C6V10 rat glioma cells are injected s.c.. Treatment continued while tumors are allowed to grow for 21 d. U87 cells (3×106/100 AL) are injected s.c. into nude mice. From day 3 after injection of tumor cells, mice are treated by micronized Palomid 529 (P529) at doses of 50 mg and 25 mg/kg/2 d i.p., respectively. Mice without drug treatment served as controls. U87 tumors are allowed to grow for 24 d. During drug treatment, tumor volumes are measured with a caliper and estimated as length×width×width×0.53. Animals are euthanized and the tumors are taken for immunohistologic and immunoblotting studies.

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

    参考文献

    Palomid 529 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 2.4604 mL 12.3022 mL 24.6045 mL 61.5112 mL
    5 mM 0.4921 mL 2.4604 mL 4.9209 mL 12.3022 mL
    10 mM 0.2460 mL 1.2302 mL 2.4604 mL 6.1511 mL
    15 mM 0.1640 mL 0.8201 mL 1.6403 mL 4.1007 mL
    20 mM 0.1230 mL 0.6151 mL 1.2302 mL 3.0756 mL
    25 mM 0.0984 mL 0.4921 mL 0.9842 mL 2.4604 mL
    30 mM 0.0820 mL 0.4101 mL 0.8201 mL 2.0504 mL
    40 mM 0.0615 mL 0.3076 mL 0.6151 mL 1.5378 mL
    50 mM 0.0492 mL 0.2460 mL 0.4921 mL 1.2302 mL
    60 mM 0.0410 mL 0.2050 mL 0.4101 mL 1.0252 mL
    80 mM 0.0308 mL 0.1538 mL 0.3076 mL 0.7689 mL
    100 mM 0.0246 mL 0.1230 mL 0.2460 mL 0.6151 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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