Topoisomerase I/II inhibitor 2
Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in researching liver cancer.
For research use only. We do not sell to patients.
- CAS No.: 2770804-58-3
- Formula: C19H16N2O4
- Molecular Weight:336.34
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Topoisomerase Isoforms
More
Biological Activity
Description
IC50 & Target
|
Topoisomerase I |
Topoisomerase II |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
36.3 μM
Compound: 1a
|
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
|
[PMID: 34802836] |
| BGC-823 | IC50 |
17.7 μM
Compound: 1a
|
Antiproliferative activity against human BGC-823 cells after 72 hrs by MTT assay
Antiproliferative activity against human BGC-823 cells after 72 hrs by MTT assay
|
[PMID: 34802836] |
| HCCLM9 | IC50 |
6.83 μM
Compound: 1a
|
Antiproliferative activity against human HCCLM9 cells after 72 hrs by MTT assay
Antiproliferative activity against human HCCLM9 cells after 72 hrs by MTT assay
|
[PMID: 34802836] |
| HCT-116 | IC50 |
64 μM
Compound: 1a
|
Antiproliferative activity against human HCT-116 cells after 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells after 72 hrs by MTT assay
|
[PMID: 34802836] |
| HepG2 | IC50 |
52 μM
Compound: 1a
|
Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
|
[PMID: 34802836] |
| HGC-27 | IC50 |
34.25 μM
Compound: 1a
|
Antiproliferative activity against human HGC-27 cells after 72 hrs by MTT assay
Antiproliferative activity against human HGC-27 cells after 72 hrs by MTT assay
|
[PMID: 34802836] |
| HL-60 | IC50 |
59.14 μM
Compound: 1a
|
Antiproliferative activity against human HL-60 cells after 72 hrs by MTT assay
Antiproliferative activity against human HL-60 cells after 72 hrs by MTT assay
|
[PMID: 34802836] |
| HT-29 | IC50 |
31 μM
Compound: 1a
|
Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay
Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay
|
[PMID: 34802836] |
| Huh-7 | IC50 |
9.82 μM
Compound: 1a
|
Antiproliferative activity against human Huh-7 cells after 72 hrs by MTT assay
Antiproliferative activity against human Huh-7 cells after 72 hrs by MTT assay
|
[PMID: 34802836] |
| L02 | IC50 |
>150 μM
Compound: 1a
|
Antiproliferative activity against human L02 cells after 72 hrs by MTT assay
Antiproliferative activity against human L02 cells after 72 hrs by MTT assay
|
[PMID: 34802836] |
| MCF7 | IC50 |
22.4 μM
Compound: 1a
|
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
|
[PMID: 34802836] |
| MDA-MB-231 | IC50 |
19.9 μM
Compound: 1a
|
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay
|
[PMID: 34802836] |
| RKO | IC50 |
47.8 μM
Compound: 1a
|
Antiproliferative activity against human RKO cells after 72 hrs by MTT assay
Antiproliferative activity against human RKO cells after 72 hrs by MTT assay
|
[PMID: 34802836] |
| SGC-7901 | IC50 |
30.76 μM
Compound: 1a
|
Antiproliferative activity against human SGC-7901 cells after 72 hrs by MTT assay
Antiproliferative activity against human SGC-7901 cells after 72 hrs by MTT assay
|
[PMID: 34802836] |
| SK-HEP1 | IC50 |
16.53 μM
Compound: 1a
|
Antiproliferative activity against human SK-HEP1 cells after 72 hrs by MTT assay
Antiproliferative activity against human SK-HEP1 cells after 72 hrs by MTT assay
|
[PMID: 34802836] |
| SW480 | IC50 |
9.04 μM
Compound: 1a
|
Antiproliferative activity against human SW480 cells after 72 hrs by MTT assay
Antiproliferative activity against human SW480 cells after 72 hrs by MTT assay
|
[PMID: 34802836] |
| U-251 | IC50 |
13.5 μM
Compound: 1a
|
Antiproliferative activity against human U-251 cells after 72 hrs by MTT assay
Antiproliferative activity against human U-251 cells after 72 hrs by MTT assay
|
[PMID: 34802836] |
In Vitro
Topoisomerase I/II inhibitor 2 (compound 1a) (0-150 μM; 72 hours) has favourable anti-proliferative activity in cancer cell lines, and better inhibitory activity on two human hepatocellular carcinoma cell lines (HuH7, LM9)[1].
Topoisomerase I/II inhibitor 2 (20 μM; 24 hours) has no damage to the DNA of HuH7 cells while some damage is noticed on LM9 cells[1].
Topoisomerase I/II inhibitor 2 (1.25-8 μM; 1-2 weeks) inhibits cell proliferation of LM9 and Huh7 in a concentration-dependent manner[1].
Topoisomerase I/II inhibitor 2 (1.25-8 μM; 24 hours) has a good inhibitory effect on the migration and invasion of LM9 and HuH7 cells with concentration-dependent manner[1].
Topoisomerase I/II inhibitor 2 (0-20 μM; 24 hours) can inhibit the expression of matrix metalloproteinases-9 (MMP-9) in LM9 and HuH7 cells[1].
Topoisomerase I/II inhibitor 2 (0-20 μM; 48 hours) inhibits cells proliferation by blocking cell cycle at the G2/M phase[1].
Topoisomerase I/II inhibitor 2 (3.5-20 μM; 48 hours) can injure mitochondrial function and induce cell apoptosis in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:LM9, HuH7, SK-hep-1, HepG2, HT-29, HCT-116, RKO, SW480, MCF-7, MDA-B-231, HGC-27, SGC-7901, BGC-823, A549, U251, HL-60, LO2[1]
-
Concentration:0-150 μM
-
Incubation Time:72 hours
-
Result:Displayed favourable anti-proliferative activity and had better inhibitory activity on two human hepatocellular carcinoma cell lines (HuH7, LM9).
-
Cell Line:LM9 and HuH7 cells[1]
-
Concentration:0, 3.75, 7.5, 15 μM in LM9; 0, 5, 10, 20 μM in HuH7
-
Incubation Time:48 hours
-
Result:Inhibited the expression of MMP-9.
-
Cell Line:LM9 and HuH7 cells[1]
-
Concentration:0, 3.75, 7.5, 15 μM in LM9; 0, 5, 10, 20 μM in HuH7
-
Incubation Time:48 hours
-
Result:Inhibited cells proliferation by blocking cell cycle at the G2/M phase.
-
Cell Line:LM9 and HuH7 cells[1]
-
Concentration:3.5, 7, 14 μM in LM9; 5, 10, 20 μM in HuH7
-
Incubation Time:48 hours
-
Result:Induced apoptosis in a dose-dependent manner.
Chemical Information
-
CAS No. 2770804-58-3
-
Molecular Weight 336.34
-
Formula C19H16N2O4
-
SMILES
CNCC1=CC2=C(OCO2)C=C1C3=CC4=C(C5=C(OCO5)C=C4)C=N3
-
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
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)