1. Cell Cycle/DNA Damage
  2. Topoisomerase
  3. Topoisomerase I inhibitor 12

Topoisomerase I inhibitor 12 (compound 12), a Camptothecin (HY-16560)-based derivative, is a potent Topoisomerase I inhibitor. Topoisomerase I inhibitor 12 shows anticancer activity.

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Topoisomerase I inhibitor 12

Topoisomerase I inhibitor 12 Chemical Structure

CAS No. : 3038811-66-1

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Description

Topoisomerase I inhibitor 12 (compound 12), a Camptothecin (HY-16560)-based derivative, is a potent Topoisomerase I inhibitor. Topoisomerase I inhibitor 12 shows anticancer activity[1].

IC50 & Target

Topoisomerase I

 

Cellular Effect
Cell Line Type Value Description References
BJ IC50
4.25 μM
Compound: 12
Cytotoxicity against human BJ cells incubated for 48 hrs by MTT assay
Cytotoxicity against human BJ cells incubated for 48 hrs by MTT assay
[PMID: 38185054]
DU-145 IC50
3.81 μM
Compound: 12
Cytotoxicity against human DU-145 cells incubated for 48 hrs by MTT assay
Cytotoxicity against human DU-145 cells incubated for 48 hrs by MTT assay
[PMID: 38185054]
HCT-116 IC50
3.67 μM
Compound: 12
Cytotoxicity against human HCT-116 cells incubated for 48 hrs by MTT assay
Cytotoxicity against human HCT-116 cells incubated for 48 hrs by MTT assay
[PMID: 38185054]
HOS IC50
1.47 μM
Compound: 12
Cytotoxicity against human HOS cells incubated for 48 hrs by MTT assay
Cytotoxicity against human HOS cells incubated for 48 hrs by MTT assay
[PMID: 38185054]
MCF7 IC50
56.4 μM
Compound: 12
Cytotoxicity against human MCF7 cells incubated for 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells incubated for 48 hrs by MTT assay
[PMID: 38185054]
MDA-MB-231 IC50
5.96 μM
Compound: 12
Cytotoxicity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay
[PMID: 38185054]
MG-63 IC50
17.94 μM
Compound: 12
Cytotoxicity against human MG-63 cells incubated for 48 hrs by MTT assay
Cytotoxicity against human MG-63 cells incubated for 48 hrs by MTT assay
[PMID: 38185054]
PANC-1 IC50
19.05 μM
Compound: 12
Cytotoxicity against human PANC-1 cells incubated for 48 hrs by MTT assay
Cytotoxicity against human PANC-1 cells incubated for 48 hrs by MTT assay
[PMID: 38185054]
PC-3 IC50
> 100 μM
Compound: 12
Cytotoxicity against human PC-3 cells incubated for 48 hrs by MTT assay
Cytotoxicity against human PC-3 cells incubated for 48 hrs by MTT assay
[PMID: 38185054]
SAOS-2 IC50
3.2 μM
Compound: 12
Cytotoxicity against human SAOS-2 cells incubated for 48 hrs by MTT assay
Cytotoxicity against human SAOS-2 cells incubated for 48 hrs by MTT assay
[PMID: 38185054]
SK-OV-3 IC50
3.48 μM
Compound: 12
Cytotoxicity against human SK-OV-3 cells incubated for 48 hrs by MTT assay
Cytotoxicity against human SK-OV-3 cells incubated for 48 hrs by MTT assay
[PMID: 38185054]
In Vitro

Topoisomerase I inhibitor 12 (compound 12) shows moderate antiproliferative activity against the MDA-MB-231, DU-145, HCT-116, SKOV-3, and SAOS-2 cancer cell lines (with IC50 values of 5.96±0.03, 3.81±1.37, 3.67±0.21, 3.48±1.02, and 3.20±0.21 µM, respectively), as well as potent activity against the HOS (osteosarcoma) cancer cell line (IC50=1.47 µM) while the potential of Topoisomerase I inhibitor 12 against fibroblast normal cells (BJ1) demonstrated a 2.89-fold selectivity (IC50=4.25 µM) against cancer cell[1].

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

Molecular Weight

402.45

Formula

C23H22N4O3

CAS No.
SMILES

O=C1N2C(N(CCN3CCOCC3)C(/C2=C\C4=CC=CC=C4)=O)=NC5=CC=CC=C51

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
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Topoisomerase I inhibitor 12
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HY-161082
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