Initial testing (stage 1) of the polyamine analog PG11047 by the pediatric preclinical testing program.

ABSTRACT:

Background

PG11047 is a novel conformationally restricted analog of the natural polyamine, spermine that lowers cellular endogenous polyamine levels and competitively inhibits natural polyamine functions leading to cancer cell growth inhibition. The activity of PG11047 was evaluated against the PPTP's in vitro and in vivo panels.

Procedures

PG11047 was evaluated against the PPTP in vitro panel using 96 hr exposure at concentrations ranging from 10 nM to 100 µM. It was tested against the PPTP in vivo panels at a dose of 100 mg/kg administered by the intraperitoneal route weekly for 6 weeks.

Results

In vitro PG11047 demonstrated a concentration-response pattern consistent with cytostatic activity. The median EC(50) for PG11047 was 71 nM. Cell lines of the Ewing sarcoma

SUBMITTER: Smith MA 

PROVIDER: S-EPMC3115432 | biostudies-literature | 2011 Aug

REPOSITORIES: biostudies-literature