Analytical and Pharmacological Studies on a New Antineoplastic Tripeptide, PTT.119
作者:
John Roboz,
John Greaves,
Mary Jane Yagi,
James F. Holland,
George Bekesi,
期刊:
Pharmacology
(Karger Available online 1985)
卷期:
Volume 30,
issue 1
页码: 52-59
ISSN:0031-7012
年代: 1985
DOI:10.1159/000138050
出版商: S. Karger AG
关键词: Tripeptide;PTT. 119;Cellular uptake;Mass spectra;Quantification;Cell kill of PTT. 119
数据来源: Karger
摘要:
The new synthetic tripeptide, p-fluoro-L-phenylalanyl-m-bis-(2-chloroethyl)- amino-L-phenylalanyl-methionine ethylester hydrochloride, PTT.l 19, an alkylating agent, is currently undergoing preclinical trials as an antineoplastic agent. The molecular composition, C29H39N4O4SCl2F, was confirmed by desorption chemical ionization mass spectrometry with accurate mass measurement. A high-performance liquid chromatographic technique was developed for the quantification of PTT.l 19 in cell culture medium and serum. Incubation of 5 × 105 mammary tumor cells (MJY-α)/ml tissue culture medium with 25 μg PTT. 119/ml for 60 min (37°C) removed 68% of the tripeptide from the medium. This corresponds to an uptake of 51 fmol PTT.119/tumor cell. Cell death, assessed 5 days after treatment, was directly proportional to the time-dependent removal of PTT.119 from the cell culture med
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