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Pediatr Blood Cancer. 2012 Jul 15;59(1):185-8. doi: 10.1002/pbc.23154. Epub 2011 Apr 29.

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

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1
Texas Tech University Health Sciences Center, Lubbock, Texas 79430-6450, USA. min.kang@ttuhsc.edu

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.

PMID:
21538821
PMCID:
PMC3154460
DOI:
10.1002/pbc.23154
[Indexed for MEDLINE]
Free PMC Article
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