| Name | TAS-103 dihydrochloride |
| Description | TAS-103 dihydrochloride (BMS-247615 dihydrochloride) is a novel anticancer agent targeting both topoisomerase (Topo) I and Topo II. |
| In vitro | The in vitro antitumor effects of TAS-103 were compared with those of other known Topo I and Topo II inhibitors. TAS-103 inhibited DNA synthesis more strongly than RNA and protein synthesis, and induced an increase of cell population in the S-G2/M phase. The cytotoxicity of TAS-103 was strongest against S-phase cells, but its cell cycle phase specificity was not clear, and depended on drug concentration and exposure time. The cytotoxicity of TAS-103 (IC50: 0.0030-0.23 microM) against various tumor cell lines was much stronger than that of VP-16 and comparable to that of SN-38. The cytotoxicity of TAS-103 seemed to be more related to the amount of protein-DNA complexes than to the accumulation of TAS-103 in the cells. P-Glycoprotein (P-gp)-mediated MDR, CDDP-resistant and 5-FU-resistant cell lines did not show cross-resistance to TAS-103. Although PC-7/CPT cells bearing a Topo I gene mutation showed cross-resistance to TAS-103, the sensitivity of P388/CPT, HT-29/CPT and St-4/CPT cells, showing decreased Topo I expression, was not changed. KB/VM4 and HT-29/Etp cells, showing decreased Topo II expression, were slightly cross-resistant to TAS-103. These results suggest that TAS-103 may act as an inhibitor of both Topo I and Topo II at the cellular level[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | H2O : 50 mg/mL (123.06 mM), Sonication is recommended.
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| Keywords | Topoisomerase | TAS-103 | TAS 103 | inhibit | TAS 103 dihydrochloride | TAS-103 Dihydrochloride | Inhibitor | TAS103 dihydrochloride | BMS-247615 Dihydrochloride | TAS103 Dihydrochloride | TAS103 | BMS-247615 | BMS 247615 | BMS 247615 Dihydrochloride | TAS 103 Dihydrochloride | BMS247615 | BMS247615 Dihydrochloride |
| Inhibitors Related | Berberine chloride | EIDD-1931 | Flumequine | Norfloxacin | Prulifloxacin | Enoxacin | Pefloxacin Mesylate | Camptothecin | Ciprofloxacin | Ciprofloxacin monohydrochloride | Irinotecan hydrochloride trihydrate | Etoposide |
| Related Compound Libraries | DNA Damage & Repair Compound Library | Bioactive Compound Library | ReFRAME Related Library | Inhibitor Library | NO PAINS Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
