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Cat. No.: HY-146504

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Topoisomerase I/II inhibitor 3

Topoisomerase I/II inhibitor 3 (compound 7) is a potent topoisomerase I (Topo I) and II (Topo II) dual inhibitor. Topoisomerase I/II inhibitor 3 can inhibit cell proliferation, invasion and migration, and induce apoptosis by inhibiting PI3K/Akt/mTOR signaling pathway. Topoisomerase I/II inhibitor 3 can be used for liver cancer research.

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

CAS No.: 2770804-74-3
Formula: C₂₄H₂₄N₂O₄
Molecular Weight:404.46

Storage:

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

Data Sheet (278 KB)

Topoisomerase I/II inhibitor 3 Chemical Structure

CAS No.: 2770804-74-3

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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
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Biological Activity

Description

IC₅₀ & Target

Topoisomerase I

Topoisomerase II

PI3K

All Topoisomerase Isoforms :

All PI3K Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	22.91 μM Compound: 7	Antiproliferative activity against human A549 cells measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells measured after 72 hrs by MTT assay	[PMID: 35462164]
BGC-823	IC₅₀	18.55 μM Compound: 7	Antiproliferative activity against human BGC-823 cells measured after 72 hrs by MTT assay Antiproliferative activity against human BGC-823 cells measured after 72 hrs by MTT assay	[PMID: 35462164]
C6	IC₅₀	12.88 μM Compound: 7	Antiproliferative activity against human C6 cells measured after 72 hrs by MTT assay Antiproliferative activity against human C6 cells measured after 72 hrs by MTT assay	[PMID: 35462164]
HCCLM9	IC₅₀	2.1 μM Compound: 7	Antiproliferative activity against human HCCLM9 cells measured after 72 hrs by MTT assay Antiproliferative activity against human HCCLM9 cells measured after 72 hrs by MTT assay	[PMID: 35462164]
HCT-116	IC₅₀	11.39 μM Compound: 7	Antiproliferative activity against human HCT-116 cells measured after 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells measured after 72 hrs by MTT assay	[PMID: 35462164]
HepG2	IC₅₀	25.84 μM Compound: 7	Antiproliferative activity against human HepG2 cells measured after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells measured after 72 hrs by MTT assay	[PMID: 35462164]
HGC-27	IC₅₀	12.37 μM Compound: 7	Antiproliferative activity against human HGC-27 cells measured after 72 hrs by MTT assay Antiproliferative activity against human HGC-27 cells measured after 72 hrs by MTT assay	[PMID: 35462164]
HT-29	IC₅₀	5.35 μM Compound: 7	Antiproliferative activity against human HT-29 cells measured after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells measured after 72 hrs by MTT assay	[PMID: 35462164]
Huh-7	IC₅₀	1.93 μM Compound: 7	Antiproliferative activity against human Huh-7 cells measured after 72 hrs by MTT assay Antiproliferative activity against human Huh-7 cells measured after 72 hrs by MTT assay	[PMID: 35462164]
L02	IC₅₀	68.03 μM Compound: 7	Cytotoxicity against human L02 cells measured after 72 hrs by MTT assay Cytotoxicity against human L02 cells measured after 72 hrs by MTT assay	[PMID: 35462164]
MGC-803	IC₅₀	19.9 μM Compound: 7	Antiproliferative activity against human MGC-803 cells measured after 72 hrs by MTT assay Antiproliferative activity against human MGC-803 cells measured after 72 hrs by MTT assay	[PMID: 35462164]
RKO	IC₅₀	17.74 μM Compound: 7	Antiproliferative activity against human RKO cells measured after 72 hrs by MTT assay Antiproliferative activity against human RKO cells measured after 72 hrs by MTT assay	[PMID: 35462164]
SGC-7901	IC₅₀	34.79 μM Compound: 7	Antiproliferative activity against human SGC-7901 cells measured after 72 hrs by MTT assay Antiproliferative activity against human SGC-7901 cells measured after 72 hrs by MTT assay	[PMID: 35462164]
SW480	IC₅₀	8.36 μM Compound: 7	Antiproliferative activity against human SW480 cells measured after 72 hrs by MTT assay Antiproliferative activity against human SW480 cells measured after 72 hrs by MTT assay	[PMID: 35462164]
U-87MG ATCC	IC₅₀	54.62 μM Compound: 7	Antiproliferative activity against human U87 cells measured after 72 hrs by MTT assay Antiproliferative activity against human U87 cells measured after 72 hrs by MTT assay	[PMID: 35462164]

In Vitro

Topoisomerase I/II inhibitor 3 (compound 7) (0-100 μM) can insert into DNA and change the topology of DNA, cause DNA damage to a certain extent^[1].
Topoisomerase I/II inhibitor 3 (0-4 μM, 24 h) inhibits HCC (hepatocellular carcinoma) cells proliferation in a dose-dependent manner, inhibits migration and invasion of LM9 and HuH7 cells by inhibiting the expression of MMP-9^[1].
Topoisomerase I/II inhibitor 3 (0-14 μM, 48 h) significantly induces the apoptosis of LM9 and HuH7 cells, and induces mitochondrial dysfunction and ROS burst in a dose-dependent manner^[1].
Topoisomerase I/II inhibitor 3 (0-7 μM, 48 h) reduces the expression of the inhibitory factor Bcl-2 and promotes the expression of mitochondria-dependent apoptosis-related proteins such as Bax, cytochrome C, cleaved-caspase-3 and cleaved-caspase-9; inhibits the phosphorylation of PI3K/Akt/mTOR signaling pathway^[1].

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

Cell Proliferation Assay

Cell Line:

HCC cells (HuH7 and LM9)^[1]
Concentration:

0, 0.5, 1, 2, and 4 μM
Incubation Time:

24 h
Result:

Inhibited HCC cells proliferation in a dose-dependent manner, with IC₅₀ values of 2.10 μM (LM9) and 1.93 μM (HuH7), respectively, and dose-dependently inhibited the formation of cell colonies.

Apoptosis Analysis

Cell Line:

LM9 and HuH7 cells^[1]
Concentration:

0, 1.8, 3.5, 7, and 14 μM
Incubation Time:

48 h
Result:

Significantly induced the apoptosis of LM9 and HuH7 cells in a concentration-dependent manner.

Western Blot Analysis

Cell Line:

LM9 and HuH7 cells^[1]
Concentration:

0, 1.8, 3.5, and 7 μM
Incubation Time:

48 h
Result:

Reduced the expression of the inhibitory factor Bcl-2 and promoted the expression of mitochondria-dependent apoptosis-related proteins such as Bax, cytochrome C, cleaved-caspase-3 and cleaved-caspase-9; inhibited the phosphorylation of PI3K/Akt/mTOR signaling pathway.

In Vivo

Topoisomerase I/II inhibitor 3 (compound 7) (male Kunming mice, 0-400 mg/kg, IP, once) causes the mice in the 400 mg/kg group die, with the LD₅₀ between 250 and 400 mg/kg^[1].

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

Animal Model:

Male Kunming mice (19-22 mg, 8 mice, 4 groups)^[1]
Dosage:

200, 250, 400 mg/kg (dissolved in 5% DMSO and castor oil)
Administration:

IP, once
Result:

Did not cause the mice in the 250 mg/kg and 200 mg/kg groups die after 2 weeks of administration, and caused the mice in the 400 mg/kg group die, with the LD₅₀ between 250 and 400 mg/kg.

Chemical Information

CAS No. 2770804-74-3
Molecular Weight 404.46
Formula C₂₄H₂₄N₂O₄
SMILES

C1(C=CC2=C3C=NC(C4=CC5=C(OCO5)C=C4CN6CCCCCC6)=C2)=C3OCO1
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 (278 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]. Deng X, Luo T, Zhang X, et al. Design, synthesis and biological evaluation of 3-arylisoquinoline derivatives as topoisomerase I and II dual inhibitors for the therapy of liver cancer. Eur J Med Chem. 2022;237:114376. [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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MOQ

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100 mg

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