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本试剂(依托泊苷磷酸酯)
仅供科研实验使用,不得用于其他用途!
简介:
货 号:LC1-E-4444
名 称:依托泊苷磷酸酯
别 名:Etoposide 4'-Phosphate Free Acid
C A S :117091-64-2
分子量:668.54
分子式:C29H33O16P
纯 度:HPLC/TLC:>99%
说 明:Storage: Store at or below -20 ºC. Solubility: Soluble in water and DMSO. Disposal: A.
文 献:The conversion of etoposide 4'-phosphate to etoposide occurs in the GI tract after oral administration. de Jong, R.S., et al. "Conversion of the prodrug etoposide phosphate to etoposide in gastric juice and bile." Br. J. Cancer 76: 1480-1483 (1997).Free etoposide inhibits topoisomerase II. A ternary complex of etoposide, DNA and the topoisomerase II enzyme forms and prevents re-ligation of the DNA strands. This results in errors in DNA synthesis and induces apoptosis of the cancer cell. Nitiss, J.L. "Targeting DNA topoisomerase II in cancer themotherapy." Nat. Rev. Cancer 9: 338-350 (2009).In in vitro studies with the H3347 human colon carcinoma cell line, etoposide 4'-phosphate was less toxic than etoposide by a factor of greater than 100. A stronger antitumor response was observed in H3347-bearing mice that were treated with a monoclonal antibody plus L6 (anticarcinoma)-alkaline phosphatase conjugate followed 18-24 hr later by etoposide 4'-phosphate when compared to treatment with etoposide 4'-phosphate or etoposide alone. Senter, P.D., et al. "Anti-tumor effects of antibody-alkaline phosphatase conjugates in combination with etoposide phosphate." Proc. Natl. Acad. Sci. USA 85: 4842-4846 (1988).Disruption of the murine multidrug resistance protein gene resulted in a two-fold increase in sensitivity to etoposide 4'-phosphate. Lorico, A., et al. "Disruption of the murine MRP (multidrug resistance protein) gene leads to increased sensitivity to etoposide (VP-16) and increased levels of glutathione." Cancer Res. 57: 5238-5242 (1997).A phase III clinical trial showed that patients with advanced small-cell lung cancer (SCLC) gained a survival benefit and improved quality of life after treatment with the combination of etoposide, carboplatin and paclitaxel. Reck, M., et al. "Efficient palliation in patients with small-cell lung cancer by a combination of paclitaxel, etoposide and carboplatin: quality of life and 6-years'-follow-up results from a randomised phase III trial." Lung Cancer 53: 67-75 (2006).
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