Merbarone
Based on 1 Customer Validation
Merbarone (NSC 336628) is an orally active inhibitor of topoisomerase II. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage without stabilizing topo II-DNA covalent complexes. Merbarone is an anticancer agent.
For research use only. We do not sell to patients.
- Purity: 99.0%
- CAS No.: 97534-21-9
- Formula: C11H9N3O3S
- Molecular Weight:263.27
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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All Topoisomerase Isoforms
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Biological Activity
topoisomerase II[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
40 μM
Compound: Merbarone
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Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
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[PMID: 29077404] |
| A549 | IC50 |
40 μM
Compound: Merbarone
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Antiproliferative activity against human A549 cells by MTT assay
Antiproliferative activity against human A549 cells by MTT assay
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[PMID: 32196342] |
| DU-145 | IC50 |
18.9 μM
Compound: Merbarone
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Antiproliferative activity against human DU145 cells after 72 hrs by MTT assay
Antiproliferative activity against human DU145 cells after 72 hrs by MTT assay
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[PMID: 29077404] |
| DU-145 | IC50 |
18.9 μM
Compound: Merbarone
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Antiproliferative activity against human DU145 cells by MTT assay
Antiproliferative activity against human DU145 cells by MTT assay
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[PMID: 32196342] |
| HeLa | IC50 |
43.8 μM
Compound: Merbarone
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Cytotoxicity against human HeLa cells
Cytotoxicity against human HeLa cells
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[PMID: 24063907] |
| HeLa | IC50 |
62.3 μM
Compound: Merbarone
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Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay
Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay
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[PMID: 29077404] |
| HeLa | IC50 |
62.3 μM
Compound: Merbarone
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Antiproliferative activity against human HeLa cells by MTT assay
Antiproliferative activity against human HeLa cells by MTT assay
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[PMID: 32196342] |
| MCF7 | IC50 |
61.6 μM
Compound: Merbarone
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Cytotoxicity against human MCF7 cells
Cytotoxicity against human MCF7 cells
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[PMID: 24063907] |
| MCF7 | IC50 |
83.9 μM
Compound: Merbarone
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Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
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[PMID: 29077404] |
| MT4 | IC50 |
12 μM
Compound: Merbarone
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Cytotoxicity against human MT4 cells
Cytotoxicity against human MT4 cells
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[PMID: 24063907] |
Merbarone (1-100 μM) inhibits L1210 cells proliferation in a concentration-dependent manner, with an IC50 of 10 μM[3].
Merbarone (10-200 μM; 10 min) inhibits DNA relaxation catalyzed by human topoisomerase IIα, with an IC50 of ～40 μM[1].
Merbarone (25-200 μM; 6 min) blocks tyopoisomerase II-mediated DNA cleavage, with an IC50 of ～50 μM[1].
Merbarone (100 μM; 6 min) inhibits topoisomerase II-mediated DNA cleavage in a global manner[1].
Merbarone (100 μM; 6 min) does not impair topoisomerase II DNA binding[1].
Merbarone (200 μM; 4-16 min) does not inhibit topoisomerase II-catalyzed ATP hydrolysis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Merbarone (124 mg/kg; daily p.o. for 9 d) has anti-tumor activity in mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 97534-21-9
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Appearance Solid
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Molecular Weight 263.27
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Formula C11H9N3O3S
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Color Pink to purple
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SMILES
O=C(C(C(N1)=O)C(NC1=S)=O)NC2=CC=CC=C2
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Synonyms
NSC 336628
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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 6 months -20°C 1 month
Solvent & Solubility
DMSO : 12.5 mg/mL (47.48 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (9.50 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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 (9.50 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (253 KB)
- English - EN (253 KB)
- Français - FR (253 KB)
- Deutsch - DE (253 KB)
- Norwegian - NO (253 KB)
- Español - ES (253 KB)
- Swedish - SV (253 KB)
- Italian - IT (253 KB)
- Korean - KR (253 KB)
- Portuguese - PT (253 KB)
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Handling Instructions (2659 KB)
References
[1]. Fortune JM, et, al. Merbarone inhibits the catalytic activity of human topoisomerase IIalpha by blocking DNA cleavage. J Biol Chem. 1998 Jul 10;273(28):17643-50. [Content Brief]
[2]. Brewer AD, et, al. 5-(N-phenylcarboxamido)-2-thiobarbituric acid (NSC 336628), a novel potential antitumor agent. Biochem Pharmacol. 1985 Jun 1;34(11):2047-50. [Content Brief]
[3]. Cooney DA, et, al. Initial mechanistic studies with merbarone (NSC 336628). Biochem Pharmacol. 1985 Sep 15;34(18):3395-8. [Content Brief]
[4]. Chen M, et, al. Differences in inhibition of chromosome separation and G2 arrest by DNA topoisomerase II inhibitors merbarone and VM-26. Cancer Res. 1995 Apr 1;55(7):1509-16. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.7984 mL | 18.9919 mL | 37.9838 mL | 94.9596 mL |
| 5 mM | 0.7597 mL | 3.7984 mL | 7.5968 mL | 18.9919 mL | |
| 10 mM | 0.3798 mL | 1.8992 mL | 3.7984 mL | 9.4960 mL | |
| 15 mM | 0.2532 mL | 1.2661 mL | 2.5323 mL | 6.3306 mL | |
| 20 mM | 0.1899 mL | 0.9496 mL | 1.8992 mL | 4.7480 mL | |
| 25 mM | 0.1519 mL | 0.7597 mL | 1.5194 mL | 3.7984 mL | |
| 30 mM | 0.1266 mL | 0.6331 mL | 1.2661 mL | 3.1653 mL | |
| 40 mM | 0.0950 mL | 0.4748 mL | 0.9496 mL | 2.3740 mL |
Merbarone Related Classifications
HY-19024 Related Classifications
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