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

  • Pediatr Blood Cancer. 2012 Jul 15;59(1):185-8. doi: 10.1002/pbc.23154.
Min H Kang  1 ,  C Patrick Reynolds ,  Peter J Houghton ,  Denise Alexander ,  Christopher L Morton ,  E Anders Kolb ,  Richard Gorlick ,  Stephen T Keir ,  Hernan Carol ,  Richard Lock ,  John M Maris ,  Amy Wozniak ,  Malcolm A Smith
Affiliations
  • 1. Texas Tech University Health Sciences Center, Lubbock, Texas 79430-6450, USA. [email protected]
PMID: 21538821 DOI: 10.1002/pbc.23154
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.

Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-14463
    Onalespib
    99.11%, Hsp90 Inhibitor
    target: HSP
    Research Areas: Cancer