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Cat. No.: HY-161082

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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.

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

CAS No.: 3038811-66-1
Formula: C₂₃H₂₂N₄O₃
Molecular Weight:402.45

Storage:

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

Data Sheet (272 KB)

Topoisomerase I inhibitor 12 Chemical Structure

CAS No.: 3038811-66-1

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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
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

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

All Topoisomerase Isoforms :

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.

Chemical Information

CAS No. 3038811-66-1
Molecular Weight 402.45
Formula C₂₃H₂₂N₄O₃
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 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]. Ahmed I. Khodair, et al. Camptothecin structure simplification elaborated new imidazo[2,1-b]quinazoline derivative as a human topoisomerase I inhibitor with efficacy against bone cancer cells and colon adenocarcinoma. European Journal of Medicinal Chemistry. 16 December 2023, 116049.

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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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100 mg

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