| Cas No.: | 174634-09-4 |
| 名称: | |
| 别名: | |
| SMILES: | CN(C)CCNC1=C2C(=C3C=CC(=O)C=C3N1)C4=CC=CC=C4C2=O.Cl.Cl |
| 分子式: | C20H21Cl2N3O2 |
| 分子量: | 406.3 |
| 纯度: | |
| 保存条件: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | |
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| In Vitro: | |
| References: | 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 . 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. |
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| References: |
MSDS
| TITLE | DOWNLOAD |
| MSDS_2402_DC8536_174634-09-4 |
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COA
| LOT NO. | DOWNLOAD |
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