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Cat. No.: HY-144774

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Topoisomerase I inhibitor 5

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.

CAS No.: 2513461-95-3
Formula: C₂₄H₂₄N₂O₂
Molecular Weight:372.46

Storage:

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

Data Sheet (275 KB)

Topoisomerase I inhibitor 5 Chemical Structure

CAS No.: 2513461-95-3

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

Topoisomerase I^[1]

All Topoisomerase Isoforms :

All DNA/RNA Synthesis Isoforms :

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.

Chemical Information

CAS No. 2513461-95-3
Molecular Weight 372.46
Formula C₂₄H₂₄N₂O₂
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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Topoisomerase I inhibitor 5

All Topoisomerase Isoforms

All DNA/RNA Synthesis Isoforms