Topoisomerase II inhibitor 6

Cat. No.: HY-146316: Ficha de datos Instrucciones de manejo
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Topoisomerase II inhibitor 6 (Compound 5), a tryptanthrin derivative, is a potent and selective inhibitor of topoisomerase II. Topoisomerase II inhibitor 6 exhibits antiproliferative activity on different tumor cell lines. Topoisomerase II inhibitor 6 blocks the cell cycle of CCRF-CEM in the G2 phase and induces DNA DSB. Topoisomerase II inhibitor 6 has the potential for the research of cancer diseases.

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Topoisomerase II inhibitor 6 Estructura química

No. CAS : 2987586-62-7

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Topoisomerase Topo I Topo II DNA gyrase

Actividad biológica
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Referencias
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Descripciòn

Cellular Effect

Cell Line	Type	Value	Description	References
CCRF-CEM	GI₅₀	1.36 μM Compound: 5	Antiproliferative activity against human CCRF-CEM cells assessed as reduction in cell viability after 72 hrs by eosin exclusion dye based light microscopic method Antiproliferative activity against human CCRF-CEM cells assessed as reduction in cell viability after 72 hrs by eosin exclusion dye based light microscopic method	[PMID: 32712536]
CCRF-CEM	IC₅₀	8.26 μM Compound: 5	Antiproliferative activity against human CCRF-CEM cells assessed as reduction in cell viability after 72 hrs by eosin exclusion dye based light microscopic method Antiproliferative activity against human CCRF-CEM cells assessed as reduction in cell viability after 72 hrs by eosin exclusion dye based light microscopic method	[PMID: 32712536]
CEM/C2	IC₅₀	9.16 μM Compound: 5	Antiproliferative activity against human CEM/C2 cells assessed as reduction in cell viability after 72 hrs by eosin exclusion dye based light microscopic method Antiproliferative activity against human CEM/C2 cells assessed as reduction in cell viability after 72 hrs by eosin exclusion dye based light microscopic method	[PMID: 32712536]
DLD-1	IC₅₀	7.13 μM Compound: 5	Antiproliferative activity against human DLD-1 cells assessed as reduction in cell viability after 72 hrs by eosin exclusion dye based light microscopic method Antiproliferative activity against human DLD-1 cells assessed as reduction in cell viability after 72 hrs by eosin exclusion dye based light microscopic method	[PMID: 32712536]
HL-60	IC₅₀	11.46 μM Compound: 5	Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability after 72 hrs by eosin exclusion dye based light microscopic method Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability after 72 hrs by eosin exclusion dye based light microscopic method	[PMID: 32712536]
HT-29	IC₅₀	9.4 μM Compound: 5	Antiproliferative activity against human HT29 cells assessed as reduction in cell viability after 72 hrs by eosin exclusion dye based light microscopic method Antiproliferative activity against human HT29 cells assessed as reduction in cell viability after 72 hrs by eosin exclusion dye based light microscopic method	[PMID: 32712536]
Jurkat	IC₅₀	18.2 μM Compound: 5	Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability after 72 hrs by eosin exclusion dye based light microscopic method Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability after 72 hrs by eosin exclusion dye based light microscopic method	[PMID: 32712536]
MCF7	IC₅₀	30.48 μM Compound: 5	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by eosin exclusion dye based light microscopic method Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by eosin exclusion dye based light microscopic method	[PMID: 32712536]

Peso molecular

334.37

Fòrmula

C₁₉H₁₈N₄O₂

No. CAS

2987586-62-7

SMILES

O=C1C2=NC3=C(C(N2C4=C1C(NCCN(C)C)=CC=C4)=O)C=CC=C3

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[1]. Catanzaro E, et al. Targeting topoisomerase II with trypthantrin derivatives: Discovery of 7-((2-(dimethylamino)ethyl)amino)indolo[2,1-b]quinazoline-6,12-dione as an antiproliferative agent and to treat cancer. Eur J Med Chem. 2020 Sep 15;202:112504. [Content Brief]