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

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

For research use only. We do not sell to patients.

Palomid 529 Chemical Structure

Palomid 529 Chemical Structure

CAS No. : 914913-88-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 55 In-stock
Solution
10 mM * 1 mL in DMSO USD 55 In-stock
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10 mg USD 80 In-stock
50 mg USD 250 In-stock
100 mg USD 375 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Palomid 529 Related Antibodies

Top Publications Citing Use of Products

    Palomid 529 purchased from MedChemExpress. 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.

    View All mTOR Isoform Specific Products:

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    mTOR mTORC1 mTORC2

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target[1]

    TORC1

     

    TORC2

     

    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].

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

    Palomid 529 Related Antibodies
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    406.43

    Formula

    C24H22O6
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    COC1=C(OCC2=CC=C(C=C2)OC)C=C3C(C4=C(C(O3)=O)C=C(C(C)O)C=C4)=C1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (246.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.47%

    COA (250 KB) LCMS (121 KB)

    Handling Instructions (2659 KB)
    References
    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.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 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
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    Palomid 529 Related Classifications

    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:

    Palomid 529914913-88-5P529Palomid529Palomid-529P 529P-529mTORApoptosisMammalian target of RapamycinInhibitorinhibitorinhibit

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