Serdemetan
Based on 3 publication(s) in Google Scholar
Serdemetan (JNJ-26854165) is a potent anticancer agent with radiosensitizing activity. Serdemetan exhibits antiproliferative activity in various p53 wild-type tumor cells. Serdemetan also antagonizes the Mdm2-HIF1α axis leading to decreased levels of glycolytic enzymes.
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- Pureté: 99.56%
- CAS No.: 881202-45-5
- Formule: C21H20N4
- Masse moléculaire:328.41
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Serdemetan
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Activité biologique
Serdemetan (0.5-50 μM; 48-72 h) inhibits cell proliferation of H460, A549, p53-WT HCT116, p53-null HCT116 and HMEC-1 cells in a dose-dependent manner[1].
Serdemetan (0.25-5 μM; 48 h) triggers cell arrests in G2/M phase of A549 cells and H460 cells[1].
Serdemetan (0.5-10 μM; 48 h) increases expression of p53 and p21 in H460, A549 and p53-WT HCT116 cells[1].
Serdemetan (0.25-10 μM; 12-14 d) affects clonogenic survival in H460, A549 p53-WT HCT116 and p53-null HCT116 cells[1].
Serdemetan (0.25-5 μM; 12-14 d) increases radiation-induced clonogenic inhibition[1].
Serdemetan (5-20 μM; 4-24 h) inhibits neovessels formation and delays scratch wound repair of HMEC-1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H460, A549, p53-WT HCT116, p53-null HCT116 and HMEC-1 cells
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Concentration:0.5-50 μM
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Incubation Time:48, 72 hours
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Result:Inhibited cell proliferation with IC50s of 3.9, 8.7, 0.97, 7.74, and 7.01 μM for H460, A549, p53-WT HCT116, p53-null HCT116 and HMEC-1 cells, respectively.
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Cell Line:H460, A549, HMEC-1, p53-WT HCT116, and p53-null HCT116 cells[1]
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Concentration:0.5 μM for A549 and p53-WT HCT11 cells; 5 μM for p53-null HCT116 and HMEC-1 cells; 10 μM for A549 cells
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Incubation Time:Treated for 24 h exposure then cells were irradiated, western blots were performed on cells arrested 24 h after irradiation
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Result:Slightly increased the expression of p53 and p21 in H460, A549, p53-WT HCT116.
Increased both p53 and p21 expression 24 h after the last drug exposure.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 881202-45-5
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Appearance Solid
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Masse moléculaire 328.41
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Formule C21H20N4
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Color Light brown to brown
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SMILES
C1(NCCC2=CNC3=C2C=CC=C3)=CC=C(C=C1)NC4=CC=NC=C4
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Synonyms
JNJ-26854165
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Biochem Pharmacol
PLCE1 enhances mitochondrial dysfunction to promote GSDME-mediated pyroptosis in doxorubicin-induced cardiotoxicity. [Abstract]2024 May:223:116142. PMID: 38499110 -
Cells
PROTAC-Mediated Targeted Degradation of MDM2 Induces Tumor-Suppressive Signaling in Osteosarcoma Cells. [Abstract]2026 Mar 5;15(5):473. PMID: 41827906 -
Toxicol Appl Pharmacol
In silico and in vitro assessment of drugs potentially causing adverse effects by inhibiting CYP17A1. [Abstract]2024 May:486:116945. PMID: 38688424
Solvant et solubilité
DMSO : 50 mg/mL (152.25 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)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.61 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.61 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Pureté et documentation
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Fiche technique (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Chargari C, et, al. Preclinical assessment of JNJ-26854165 (Serdemetan), a novel tryptamine compound with radiosensitizing activity in vitro and in tumor xenografts. Cancer Lett. 2011 Dec 22;312(2):209-18. [Content Brief]
[2]. Lehman JA, et, al. Serdemetan antagonizes the Mdm2-HIF1α axis leading to decreased levels of glycolytic enzymes. PLoS One. 2013 Sep 6;8(9):e74741. [Content Brief]
[3]. Jones RJ, et, al. The novel anticancer agent JNJ-26854165 induces cell death through inhibition of cholesterol transport and degradation of ABCA1. J Pharmacol Exp Ther. 2013 Sep;346(3):381-92. [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 | 3.0450 mL | 15.2249 mL | 30.4497 mL | 76.1244 mL |
| 5 mM | 0.6090 mL | 3.0450 mL | 6.0899 mL | 15.2249 mL | |
| 10 mM | 0.3045 mL | 1.5225 mL | 3.0450 mL | 7.6124 mL | |
| 15 mM | 0.2030 mL | 1.0150 mL | 2.0300 mL | 5.0750 mL | |
| 20 mM | 0.1522 mL | 0.7612 mL | 1.5225 mL | 3.8062 mL | |
| 25 mM | 0.1218 mL | 0.6090 mL | 1.2180 mL | 3.0450 mL | |
| 30 mM | 0.1015 mL | 0.5075 mL | 1.0150 mL | 2.5375 mL | |
| 40 mM | 0.0761 mL | 0.3806 mL | 0.7612 mL | 1.9031 mL | |
| 50 mM | 0.0609 mL | 0.3045 mL | 0.6090 mL | 1.5225 mL | |
| 60 mM | 0.0507 mL | 0.2537 mL | 0.5075 mL | 1.2687 mL | |
| 80 mM | 0.0381 mL | 0.1903 mL | 0.3806 mL | 0.9516 mL | |
| 100 mM | 0.0304 mL | 0.1522 mL | 0.3045 mL | 0.7612 mL |
Serdemetan Related Classifications
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