Initial testing (Stage 1) of AT13387, an HSP90 inhibitor, by the pediatric preclinical testing program.

Journal Article

AT13387, a non-geldanamycin inhibitor of heat-shock protein 90 (HSP90), was tested against the PPTP in vitro panel (1.0 nM to 10 µM) and against the PPTP in vivo panels (40 or 60 mg/kg) administered orally twice weekly. In vitro AT13387 showed a median EC(50) value of 41 nM and exhibited activity consistent with a cytotoxic effect. In vivo AT13387 induced significant differences in EFS distribution compared to controls in 17% evaluable solid tumor xenografts, but in none of the ALL xenografts. No objective tumor responses were observed. In vivo AT13387 demonstrated only modest single agent activity.

Full Text

Duke Authors

Cited Authors

  • Kang, MH; Reynolds, CP; Houghton, PJ; Alexander, D; Morton, CL; Kolb, EA; Gorlick, R; Keir, ST; Carol, H; Lock, R; Maris, JM; Wozniak, A; Smith, MA

Published Date

  • July 15, 2012

Published In

Volume / Issue

  • 59 / 1

Start / End Page

  • 185 - 188

PubMed ID

  • 21538821

Electronic International Standard Serial Number (EISSN)

  • 1545-5017

Digital Object Identifier (DOI)

  • 10.1002/pbc.23154

Language

  • eng

Conference Location

  • United States