Cas No.: | 174634-08-3 |
Synonyms: | BMS-247615; TAS103; TAS 103; BMS247615; BMS 247615, BMS-247615; TAS103; TAS 103; BMS247615; BMS 247615 |
SMILES: | O=C(C1=C2C3=CC=C(O)C=C3N=C1NCCN(C)C)C4=C2C=CC=C4 |
Formula: | C20H19N3O2 |
M.Wt: | 333.38 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | TAS-103(BMS-247615) is a dual inhibitor of topoisomerase-I (topo-I) and topoisomerase-II (topoII). IC50 value: Target: Topoisomerase 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 . 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 the detailed information of TAS-103 HCL, the solubility of TAS-103 HCL in water, the solubility of TAS-103 HCL in DMSO, the solubility of TAS-103 HCL in PBS buffer, the animal experiment (test) of TAS-103 HCL, the cell expriment (test) of TAS-103 HCL, the in vivo, in vitro and clinical trial test of TAS-103 HCL, the EC50, IC50,and affinity,of TAS-103 HCL, Please contact DC Chemicals. |