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The antitumor agent 3-bromopyruvate has a short half-life at physiological conditions

Authors
Journal
Biochemical and Biophysical Research Communications
0006-291X
Publisher
Elsevier
Publication Date
Volume
452
Issue
1
Identifiers
DOI: 10.1016/j.bbrc.2014.08.066
Keywords
  • Alkylating Agent
  • 3-Bromopyruvate
  • Cancer Therapy
  • 3-Hydroxypyruvate
  • Tumor
  • Ketone Hydration
Disciplines
  • Biology

Abstract

Abstract Clinical research is currently exploring the validity of the anti-tumor candidate 3-bromopyruvate (3-BP) as a novel treatment for several types of cancer. However, recent publications have overlooked rarely-cited earlier work about the instability of 3-BP and its decay to 3-hydroxypyruvate (3-HP) which have obvious implications for its mechanism of action against tumors, how it is administered, and for precautions when preparing solutions of 3-BP. This study found the first-order decay rate of 3-BP at physiological temperature and pH has a half-life of only 77min. Lower buffer pH decreases the decay rate, while choice of buffer and concentration do not affect it. A method for preparing more stable solutions is also reported.

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