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Topoisomerase II inhibitor 18 2382959-65-9

Topoisomerase II inhibitor 18 2382959-65-9

CAS No.: 2382959-65-9

Topoisomerase II inhibitor 18 (Compound IV) is a quinoxaline derivative that inhibits topoisomerase II with an IC50 of 7
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Topoisomerase II inhibitor 18 (Compound IV) is a quinoxaline derivative that inhibits topoisomerase II with an IC50 of 7.5 μM. Topoisomerase II inhibitor 18 inhibits the proliferation of PC-3 cells, arrests the cell cycle at the S phase and induces apoptosis. Topoisomerase II inhibitor 18 has anticancer activity.

Physicochemical Properties


Molecular Formula C20H21N3OS
Molecular Weight 351.47
CAS # 2382959-65-9
SMILES

S(C1=NC2C=CC=CC=2N=C1C1C=CC=CC=1)CCC(=O)NCCC

Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


Targets Topoisomerase II 7.5 μM (IC50)
ln Vitro Topoisomerase II inhibitor 18 (0-100 μM) inhibits the proliferation of cancer cells PC-3 and HepG2 with IC50 values of 2.11 and 11.03 μM, respectively, and shows no significant cytotoxicity to normal Vero cells (IC50 is 23.12 μM)[1].
ln Vivo Topoisomerase II inhibitor 18 (5 mg/kg, intramuscular injection for 21 days) has antitumor activity in the Ehrlich solid tumor model of albino mice and has renal protective effects [1].
Cell Assay Western Blot Analysis[1]
Cell Types: PC-3 Tested
Tested Concentrations: 0-100 μM
Incubation Duration: 48 h
Experimental Results: Increased levels of p53, cleaved caspase-3 and cleaved caspase-8. Decreased levels of Bcl-2.

Cell Proliferation Assay[1]
Cell Types: HepG2, PC-3 Tested
Tested Concentrations: 0-100 μM
Incubation Duration: 48 h
Experimental Results: Inhibited proliferations of PC-3 and HepG2
Animal Protocol Animal/Disease Models: Ehrlich solid tumor bearing albino mice[1]
Doses: 5 mg/kg
Route of Administration: i.m. for 21 days
Experimental Results: Inhibited tumor growth.
References

[1]. A quinoxaline-based derivative exhibited potent and selective anticancer activity with apoptosis induction in PC-3 cells through Topo II inhibition. J Biomol Struct Dyn. 2024 Mar 14:1-19.


Solubility Data


Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.8452 mL 14.2260 mL 28.4519 mL
5 mM 0.5690 mL 2.8452 mL 5.6904 mL
10 mM 0.2845 mL 1.4226 mL 2.8452 mL
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.