Merbarone (Synonyms: NSC 336628)

Name: Merbarone
Brand: MedChemExpress
SKU: HY-19024
Rating: 4.5 (1 reviews)

Cat. No.: HY-19024 Purity: ≥99.0%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

Merbarone Chemical Structure

CAS No. : 97534-21-9

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 88	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 88	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 55	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 85	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 160	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 275	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 460	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Topoisomerase Topo I Topo II

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

topoisomerase II^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	40 μM Compound: Merbarone	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 29077404]
A549	IC₅₀	40 μM Compound: Merbarone	Antiproliferative activity against human A549 cells by MTT assay Antiproliferative activity against human A549 cells by MTT assay	[PMID: 32196342]
DU-145	IC₅₀	18.9 μM Compound: Merbarone	Antiproliferative activity against human DU145 cells after 72 hrs by MTT assay Antiproliferative activity against human DU145 cells after 72 hrs by MTT assay	[PMID: 29077404]
DU-145	IC₅₀	18.9 μM Compound: Merbarone	Antiproliferative activity against human DU145 cells by MTT assay Antiproliferative activity against human DU145 cells by MTT assay	[PMID: 32196342]
HeLa	IC₅₀	62.3 μM Compound: Merbarone	Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay	[PMID: 29077404]
HeLa	IC₅₀	62.3 μM Compound: Merbarone	Antiproliferative activity against human HeLa cells by MTT assay Antiproliferative activity against human HeLa cells by MTT assay	[PMID: 32196342]
MCF7	IC₅₀	83.9 μM Compound: Merbarone	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 29077404]

In Vitro

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.

In Vivo

Merbarone (50 mg/kg; daily i.p. for 5 d) achieves a maximum increased life span (ILS) of 101% in P388 murine leukemia^[2].
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.

Molecular Weight

263.27

Formula

C₁₁H₉N₃O₃S

CAS No.

97534-21-9

Appearance

Solid

Color

Pink to purple

SMILES

O=C(C(C(N1)=O)C(NC1=S)=O)NC2=CC=CC=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.7984 mL	18.9919 mL	37.9838 mL
5 mM	0.7597 mL	3.7984 mL	7.5968 mL
10 mM	0.3798 mL	1.8992 mL	3.7984 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, 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Protocol 1

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.
Protocol 2

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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: 99.49%

Select Batch:

Data Sheet (275 KB) SDS (253 KB)

COA (250 KB) HNMR (243 KB) RP-HPLC (185 KB) MS (178 KB) Elemental Analysis Report (109 KB)

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

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

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:

Merbarone97534-21-9NSC 336628NSC336628NSC-336628TopoisomerasecatalytictopoisomeraseIIDNAcleavageanticancerInhibitorinhibitorinhibit

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Merbarone (Synonyms: NSC 336628)

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Merbarone Related Antibodies

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Complete Stock Solution Preparation Table

Merbarone Related Classifications

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