CAY10744 is a topoisomerase II-alpha poison.1 It inhibits topoisomerase II-alpha by 78.9% when used at a concentration of 20 µM. CAY10744 is selective for topoisomerase II-alpha over topoisomerase I providing 100 and 0% inhibition, respectively, at 100 µM. It inhibits proliferation of HCT15 colon, T47D breast, DU145 prostate, and HeLa cervical cancer cells (IC50s = 0.014, 0.00267, 0.072, and 2.46 µM, respectively). CAY10744 induces apoptosis in T47D cells when used at concentrations of 10 and 30 µM. CAY10744 (12 mg/kg per day) reduces tumor growth in an MDA-MB-231 orthotopic mouse model of breast cancer.
Molekulargewicht:
385.84
CAS Nummer:
[2375613-31-1]
Formel:
C24H16ClNO2
Target-Kategorie:
Topoisomerase|||Others
T36195
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