Initial testing (Stage 1) of AT13387, an HSP90 inhibitor, by the pediatric preclinical testing program
Year: 2011
Type: article
Abstract: 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.
Source: Pediatric Blood & Cancer
DOI: 10.1002/pbc.23154
Institutions: Texas Tech University, Texas Tech University Health Sciences Center, Nationwide Children's Hospital, St. Jude Children's Research Hospital, Alfred I. duPont Hospital for Children, Children's Hospital at Montefiore, Duke University, Duke Medical Center, Children's Cancer Institute Australia, Children's Hospital of Philadelphia, University of Pennsylvania, National Institutes of Health, National Cancer Institute
Language: English
Topic: Heat shock proteins research
Subfield: Molecular Biology
Domain: Life Sciences
Open Access status: green
OpenAlex ID: W2113312886