Catalog No.: PC-22288Not For Human Use, Lab Use Only.
Genz-644282 is a potent, non-camptothecin topoisomerase I (Top1) inhibitor, shows potent activities against a panel of human tumor cell lines with IC50 of 1.8 nM-1.8 uM.
Genz-644282 is a potent, non-camptothecin topoisomerase I (Top1) inhibitor, shows potent activities against a panel of human tumor cell lines with IC50 of 1.8 nM-1.8 uM. Genz-644282 suppresses the PPTP cell lines mean IC50 value of 1.2 nM. Genz-644282 (0.1 μM) induces γH2AX foci in human colon cancer HCT116 cells and breast cancer MCF7 cells. Genz-644282 is not a substrate for the multidrug resistance gene 1 (MDR1) and breast cancer resistance protein (BCRP) efflux pumps, contrary to the camptothecins. Administration of Genz-644282 (1.7 mg/kg) produced a TGD of 23 days in mice bearing 786-O tumors compared with a TGD of 16 days after administration of irinotecan (60 mg/kg), with maximum T/Cs of 8.7% and 20.7%, respectively.
