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

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

Affiliation

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

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-14463
    99.62%, Hsp90 Inhibitor
    HSP