Initial testing (stage 1) of the investigational mTOR kinase inhibitor MLN0128 by the pediatric preclinical testing program

Min H. Kang, C. Patrick Reynolds, John M. Maris, Richard Gorlick, E. Anders Kolb, Richard Lock, Hernan Carol, Stephen T. Keir, Jianrong Wu, Dmitry Lyalin, Raushan T. Kurmasheva, Peter J. Houghton, Malcolm A. Smith

Research output: Contribution to journalArticle

14 Scopus citations

Abstract

MLN0128 is an investigational small molecule ATP-competitive inhibitor of the serine/threonine kinase mTOR. MLN0128 was tested against the in vitro panel at concentrations ranging from 0.1nM to 1μM and against the PPTP in vivo panels at a dose of 1mg/kg administered orally daily×28. In vitro the median relative IC50 concentration was 19nM. In vivo MLN0128 induced significant differences in EFS in 24/31 (77%) solid tumor models, but 0/7 ALL xenografts. The modest activity observed for MLN0128 against the PPTP preclinical models is similar to that previously reported for another TOR kinase inhibitor.

Original languageEnglish (US)
Pages (from-to)1486-1489
Number of pages4
JournalPediatric Blood and Cancer
Volume61
Issue number8
DOIs
StatePublished - Jan 1 2014

Keywords

  • Developmental therapeutics
  • MTOR inhibitor
  • Preclinical testing

ASJC Scopus subject areas

  • Pediatrics, Perinatology, and Child Health
  • Hematology
  • Oncology

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    Kang, M. H., Reynolds, C. P., Maris, J. M., Gorlick, R., Kolb, E. A., Lock, R., Carol, H., Keir, S. T., Wu, J., Lyalin, D., Kurmasheva, R. T., Houghton, P. J., & Smith, M. A. (2014). Initial testing (stage 1) of the investigational mTOR kinase inhibitor MLN0128 by the pediatric preclinical testing program. Pediatric Blood and Cancer, 61(8), 1486-1489. https://doi.org/10.1002/pbc.24989