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Chemical Structure : Genz-644282
CAS No.: 529488-28-6
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $88 | In stock | |
| 10 mg | $138 | In stock | |
| 50 mg | $298 | In stock | |
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| 100 mg | Get quote |
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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.
| M.Wt | 407.43 | |
| Formula | C22H21N3O5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
2,3-Dimethoxy-12-(2-(methylamino)ethyl)-[1,3]dioxolo[4',5':4,5]benzo[1,2-h]benzo[c][1,6]naphthyridin-13(12H)-one |
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1. Kurtzberg LS, et al. Clin Cancer Res. 2011 May 1;17(9):2777-87.
2. Sooryakumar D, et al. Mol Cancer Ther. 2011 Aug;10(8):1490-9.
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