Molecular Formula | C20H21Cl2N3O2 |
Molar Mass | 406.30564 |
Solubility | H2O: 15.3 mg/mL |
Storage Condition | under inert gas (nitrogen or Argon) at 2-8°C |
In vitro study | TAS-103 is a dual inhibitor of DNA topoisomerase I/II. TAS-103 (0.1-10 μM) is active on CCRF-CEM cells, with an IC 50 value of 5 nM. TAS-103 (0.1 μM) significantly increases levels of topo IIα FITC immunofluorescence in individual CCRF-CEM cells. TAS-103 (0.01-1 μM) is highly cytotoxic to Lewis lung carcinoma (LLC) cells, and Liposomal TAS-103 is almost as active as free TAS-103. TAS-103 inhibits the viability of HeLa cells, with an IC 50 of 40 nM. TAS-103 (10 μM) disrupts signal recognition particle (SRP) complex formation, and induces destabilization of SRP14 and SRP19 and its eventual degradation. |
In vivo study | TAS-103 (30 mg/kg, i.v.) causes significant tumor growth suppression in mice bearing Lewis lung carcinoma (LLC) cells, without obvious body weight loss, and the liposomal TAS-103 is more active than free TAS-103. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.461 ml | 12.306 ml | 24.612 ml |
5 mM | 0.492 ml | 2.461 ml | 4.922 ml |
10 mM | 0.246 ml | 1.231 ml | 2.461 ml |
5 mM | 0.049 ml | 0.246 ml | 0.492 ml |