Palomid 529
Based on 4 publication(s) in Google Scholar
Palomid 529 is a potent inhibitor of mTORC1 and mTORC2 complexes.
For research use only. We do not sell to patients.
- Purity : 99.37%
- CAS No.: 914913-88-5
- Formula: C24H22O6
- Molecular Weight:406.43
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Palomid 529
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Customer Validation & Images
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Biological Activity
Description
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. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 914913-88-5
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Appearance Solid
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Molecular Weight 406.43
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Formula C24H22O6
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Color White to off-white
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SMILES
COC1=C(OCC2=CC=C(C=C2)OC)C=C3C(C4=C(C(O3)=O)C=C(C(C)O)C=C4)=C1
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Synonyms
P529
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Front Pharmacol
CC-223, NSC781406, and BGT226 Exerts a Cytotoxic Effect Against Pancreatic Cancer Cells via mTOR Signaling. [Abstract]2020 Nov 11:11:580407. PMID: 33343350 -
Molecules
In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. [Abstract]2020 Apr 23;25(8):1980. PMID: 32340370 -
Biochem Biophys Res Commun
2018 Mar 4;497(2):499-505. PMID: 29432734
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.
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (283 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Handling Instructions (2659 KB)
References
[1]. Xue Q, et al. Palomid 529, a novel small-molecule drug, is a TORC1/TORC2 inhibitor that reduces tumor growth, tumor angiogenesis, and vascular permeability. Cancer Res, 2008, 68(22), 9551-9557. [Content Brief]
[2]. Weinberg MA, et al. RES-529: a PI3K/AKT/mTOR pathway inhibitor that dissociates the mTORC1 and mTORC2 complexes. Anticancer Drugs. 2016 Jul;27(6):475-87. [Content Brief]
[3]. Gravina GL, et al. The TORC1/TORC2 inhibitor, Palomid 529, reduces tumor growth and sensitizes to docetaxel andcisplatin in aggressive and hormone-refractory prostate cancer cells. Endocr Relat Cancer. 2011 Jul 1;18(4):385-400. [Content Brief]
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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