Pediatr Blood Cancer. 2011 Apr 29. doi: 10.1002/pbc.23154. [Epub ahead of print]

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

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.

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Texas Tech University Health Sciences Center, Lubbock, Texas. 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. Pediatr Blood Cancer © 2011 Wiley-Liss, Inc.

PMID:: 21538821; [PubMed - as supplied by publisher]
PMCID:: PMC3154460; [Available on 2012/10/29]

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Initial testing (Stage 1) of AT13387, an HSP90 inhibitor, by the pediatric precl...
Initial testing (Stage 1) of AT13387, an HSP90 inhibitor, by the pediatric preclinical testing program.
Pediatr Blood Cancer. 2011 Apr 29. doi: 10.1002/pbc.23154. [Epub ahead of print]

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

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