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  3. Merbarone

Merbarone (Synonyms: NSC 336628)

目录号: HY-19024
产品使用指南

Merbarone (NSC 336628) 是一种具有口服活性的拓扑异构酶 II (topoisomerase II) 抑制剂。Merbarone 的主要作用是阻断拓扑异构酶 II 介导的 DNA 切割。Merbarone 具有抗肿瘤功效。

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Merbarone Chemical Structure

Merbarone Chemical Structure

CAS No. : 97534-21-9

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Description

Merbarone (NSC 336628) is an orally active inhibitor of topoisomerase II. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage. Merbarone is an anticancer agent[1][2].

IC50 & Target

topoisomerase II[1]

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].

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].

Molecular Weight

263.27

Formula

C₁₁H₉N₃O₃S

CAS No.

97534-21-9

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

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • 摩尔计算器

  • 稀释计算器

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

MerbaroneNSC 336628NSC336628NSC-336628TopoisomerasecatalytictopoisomeraseIIDNAcleavageanticancerInhibitorinhibitorinhibit

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Merbarone
目录号:
HY-19024
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