tas-103-dihydrochloride

Description: TAS-103 dihydrochloride (also known as BMS-247615) is a potent and dual inhibitor of DNA topoisomerase I/II. It is a quinoline derivative that displays antitumor activity in murine and human tumor models. TAS-103 is active on CCRF-CEM cells with an IC50 value of 5 nM. TAS-103 at 0.1 uM significantly increases levels of topo IIalpha FITC immunofluorescence in individual CCRF-CEM cells. TAS-103 inhibits the viability of HeLa cells, with an IC50 of 40 nM. TAS-103 at 10 uM disrupts signal recognition particle (SRP) complex formation, and induces destabilization of SRP14 and SRP19 and its eventual degradation. Although TAS-103 has been reported to be a potent topoisomerase II poison. However, other studies have indicated that cellular susceptibility to TAS-103 is not correlated with topoisomerase II expression.

References: Biochem Pharmacol. 2000 Sep 15; 60(6):817-21; Mol Pharmacol. 2008 Mar; 73(3):987-94. Epub 2007 Dec 18.

Related CAS#: 174634-09-4 (diHCl salt); 174634-08-3 (free base)