TAS-103 2Hcl(BMS-247615 2Hcl) is a dual inhibitor of topoisomerase-I (topo-I) and topoisomerase-II (topoII).
Product Name: TAS-103 2HCl |Catalog Number: DC8536 |CAS 174634-09-4 |Other names: |Chemical Name: |Molecule Formular: C20H21Cl2N3O2 |MW: 406.3
TAS-103 2Hcl(BMS-247615 2Hcl) is a dual inhibitor of topoisomerase-I (topo-I) and topoisomerase-II (topoII).
in vitro: TAS-103 was effective in inhibiting in vitro proliferation of human SCLC (SBC-3 and H69) cells and their drug-resistant variants SBC-3/ADM or SBC-3/CDDP and H-69/VP, respectively. SBC-3/ADM and H-69/VP expressed high P-gp, whereas SBC-3/CDDP did not. TAS-103 disrupts SRP complex formation and reduces the amount of SRP14 and SRP19. TAS-103 treatment and RNAi-mediated knockdown of SRP54 or SRP14 promoted accumulation of the exogenously expressed chimeric protein interleukin-6-FLAG inside cells. In 13 human cancer cell lines, MGMT expression correlated with IC50 for TAS-103, whereas gamma-GCS expression inversely correlated with the IC50 value, suggesting MGMT may work to decrease TAS-103 activity but gamma-GCS may increase it.
in vivo: TAS-103 also effectively reduced the tumor growth (more than 50% inhibition) of the parental as well as MDR SCLC cells grown SC in nude mice [1]. Thirty-two patients were treated with escalating doses (50 to 200 mg/m(2)) of TAS-103, administered intravenously over 1 hour each week for 3 weeks. Pharmacokinetic analysis was performed at the 130-, 160-, and 200-mg/m(2) dose levels.
For research and scientific purpose only, not for human use.
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