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Chinese Journal of Clinical Pharmacology and Therapeutics ›› 2005, Vol. 10 ›› Issue (6): 697-700.

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Antitumor effects of novel thymidylate synthase inhibitor ZD1694 in vitro and in vivo

LI Ling, YANG Su-rong, YAO Ming-hui   

  1. Department of Pharmacology, Shanghai Medical College, Fudan University, Shanghai 200032, China
  • Received:2004-07-05 Revised:2005-03-19 Online:2005-06-26 Published:2020-11-12

Abstract: AIM: To observe the inhibitory effects of ZD1694 on the growth of S180 sarcoma cells in mice and investigate the effects of ZD1694 on the proliferation of gastric gland carcinoma SGC-7901 cell lines in vitro. METHODS: The tumor mice models were administered (ip) with ZD1694 at the different dose levels in one day or five consecutive days. The tumor weights were measured after the mice were slaughtered and the antitumor rates were calculated. In addition, MTT assay and flow cytometry were used for testing the effects of ZD1694 on SGC-7901 cell lines. RESULTS: The growth of S180 sarcoma cells in mice was inhibited by ZD1694.The order of the antitumor rates in different groups were listed as 200 mg·kg-1 × 1 d > 100 mg·kg-1 × 1 d > 40 mg·kg-1·d-1 × 5 d > 50 mg·kg-1 × 1 d > 20 mg·kg-1·d-1 ×5 d >10 mg·kg-1·d-1 ×5 d. The in-hibitory rate of ZD1694(0.001-1 000 mmol·L-1) on SGC-7901 cells were increased in concentration and timedependent manner. The cell numbers in G0-G1 phase in SGC-7901 cells were raised by ZD1694 as well. CONCLUSION: ZD1694 can take obvious antitumor effects on S180-bearing mice. The antitumor rate of ZD1694 is in a dose-dependent manner, and it is higher when the total dosage is administered in one day than that the total dosage was divided into 5 consecutive days. ZD1694 can inhibit the growth of SGC-7901 cells and block the cells in G1 phase in vitro.

Key words: ZD1694, tumor-bearing mice, SGC-7901 gastric gland carcinoma cell line, MTT assay, flow cytometry

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