Initial testing (stage 1) of the Akt inhibitor GSK690693 by the pediatric preclinical testing program.

ABSTRACT:

Background

GSK690693 is a small molecule ATP-competitive inhibitor of the pro-survival kinase Akt. Since Akt regulates multiple downstream targets including transcription factors, glycogen synthase 3, the pro-apoptotic protein Bad, as well as MDM2 and mTORC1, it was tested against the in vitro and in vivo panels of the Pediatric Preclinical Testing Program (PPTP).

Procedures

GSK690693 was tested in vitro at concentrations from 1 nM to 10 µM, and against the in vivo panel of xenografts at a dose of 30 mg/kg daily × 5 for 6 consecutive weeks. Three measures of in vivo antitumor activity were used: (1) an objective response measure modeled after the clinical setting; (2) a treated to control (T/C) tumor volume measure; and (3) a time to event measure based on the median event-f

SUBMITTER: Carol H 

PROVIDER: S-EPMC2965797 | biostudies-literature | 2010 Dec

REPOSITORIES: biostudies-literature