Topoisomerase I inhibitor 5

Cat. No.: HY-144774: FAQs
Data Sheet Handling Instructions

Molarity Calculator

Topoisomerase I inhibitor 5 is an effective topoisomerase inhibitor with IC₅₀ value of. Topoisomerase I inhibitor 5 can interfere with DNA and significantly inhibit the activity of Topoisomerase I. Topoisomerase I inhibitor 5 can arrest cell cycle at the G1 phase and induce MCF-7 cells apoptosis. Topoisomerase I inhibitor 5 has potency in reversing P-gp-mediated resistance to Adriamycin.

For research use only. We do not sell to patients.

Topoisomerase I inhibitor 5 Chemical Structure

CAS No. : 2513461-95-3

Size		Stock
MOQ		Minimum order quantity
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote
Other size		Get quote

Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

View All Topoisomerase Isoform Specific Products:

View All Isoforms

Topoisomerase Topo I Topo II

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Topoisomerase I^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	2.39 μM Compound: 14	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay Antiproliferative activity against human A549 cells after 48 hrs by MTT assay	[PMID: 35339100]
HepG2	IC₅₀	4.88 μM Compound: 14	Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 35339100]
L02	IC₅₀	36.52 μM Compound: 14	Antiproliferative activity against human L02 cells after 48 hrs by MTT assay Antiproliferative activity against human L02 cells after 48 hrs by MTT assay	[PMID: 35339100]
MCF7	IC₅₀	1.32 μM Compound: 14	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 35339100]
MDA-MB-231	IC₅₀	2.42 μM Compound: 14	Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay	[PMID: 35339100]
NCI/ADR-RES	IC₅₀	0.9 μM Compound: 14	Reversal of multidrug resistant activity in human MCF7/ADR cells after 48 hrs by MTT assay Reversal of multidrug resistant activity in human MCF7/ADR cells after 48 hrs by MTT assay	[PMID: 35339100]
NCI/ADR-RES	IC₅₀	7.64 μM Compound: 14	Antiproliferative activity against human MCF7/ADR cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7/ADR cells after 48 hrs by MTT assay	[PMID: 35339100]

In Vitro

Topoisomerase I inhibitor 5 (compound 14) (0-50 μM; 48 hours) exhibits antiproliferation activity against cancer cell lines and lower cytotoxicity in normal cells^[1].
Topoisomerase I inhibitor 5 (2-8 μM; 24 hours) induces MCF-7 cell cycle arrest at the G1 phase^[1].
Topoisomerase I inhibitor 5 (2-8 μM; 48 hours) increases the apoptotic rate of MCF-7/ADR and MCF-7 cells^[1].
Topoisomerase I inhibitor 5 (1.5-6 μM; 24 hours) increases the expression degree of cleaved-caspase-3 and cleaved-PARP in MCF-7; down-regulates the level of anti-apoptotic protein, up-regulates the levels of pro-apoptotic proteins in MCF-7/ADR^[1].
Topoisomerase I inhibitor 5 (0.1 μM; 24 hours) induces cell apoptosis by promoting the accumulation of ROS in MCF-7/ADR cell^[1].
Topoisomerase I inhibitor 5 (10 μg/ml; 24 hours) increases the accumulation of the ADR and Rh123 in MCF-7/ADR cells^[1].
Topoisomerase I inhibitor 5 (5, 10 and 20 μM; 24 hours) reduces the expression degree of P-gp by 14.95% and 18.10% in MCF-7/ADR cells at 10 and 20 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line:	A549, HepG-2, MCF-7, MDA-MB-231, MCF-7/ADR and LO2 cells^[1]
Concentration:	0-50 μM
Incubation Time:	48 hours
Result:	Exhibited antiproliferation activity against cancer cell lines, with IC₅₀s of 2.39 ± 0.23 μM, 4.88 ± 0.29 μM, 1.32 ± 0.14 μM, 7.64 ± 0.35 μM and 2.42 ± 0.14 μM in A549, HepG-2, MCF-7, MDA-MB-231, MCF-7/ADR, respectively; and has lower cytotoxicity in LO2 cells with IC₅₀ of 36.52 ± 2.36 μM.

Cell Cycle Analysis

Cell Line:	MCF-7^[1]
Concentration:	2, 4 and 8 μM
Incubation Time:	24 hours
Result:	Induced MCF-7 cell cycle arrest at the G1 phase.

Apoptosis Analysis

Cell Line:	MCF-7 and MCF-7/ADR cells^[1]
Concentration:	2, 4 and 8 μM
Incubation Time:	48 hours
Result:	Induced apoptosis in a dose-dependent manner in MCF-7 cells, and increased the apoptotic rate of the cells from 2.8% to 15.2% in MCF-7/ADR.

Western Blot Analysis

Cell Line:	MCF-7^[1]
Concentration:	1.5, 3 and 6 μM in MCF-7; 5, 10, and 20 μM in MCF-7/ADR
Incubation Time:	24 hours
Result:	Increased the expression degree of cleaved-caspase-3 and cleaved-PARP in MCF-7; down-regulated the level of anti-apoptotic protein bcl-2, up-regulated the levels of pro-apoptotic proteins bax and bad in MCF-7/ADR.

In Vivo

Topoisomerase I inhibitor 5 (1 mg/kg and 10 mg/kg; IV; every two days, for 21 days) decreases the tumor growth significantly^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Bal b/c nude mice (injected with 106 MCF-7 cells in the left flank for 7 days)^[1]
Dosage:	1 mg/kg and 10 mg/kg
Administration:	IV; every two days, for 21 days
Result:	Decreased the tumor growth significantly and the tumor inhibition ratio reached to 32.4% at 1 mg/kg and 7.2% at 10 mg/kg.

Molecular Weight

372.46

Formula

C₂₄H₂₄N₂O₂

CAS No.

2513461-95-3

SMILES

O=C(C1=CC=CC=C12)C3=CC=C(OCCN4C(C)CCCC4)C5=CC=NC2=C53

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Zhong H, Zhao M, Wu C, Zhang J, Chen L, Sun J. Development of oxoisoaporphine derivatives with topoisomerase I inhibition and reversal of multidrug resistance in breast cancer MCF-7/ADR cells. Eur J Med Chem. 2022;235:114300. [Content Brief]