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

Journal Article

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 0.1 nM to 1 μM and against the PPTP in vivo panels at a dose of 1 mg/kg administered orally daily × 28. In vitro the median relative IC(50) concentration was 19 nM. 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.

Full Text

Duke Authors

Cited Authors

  • Kang, MH; Reynolds, CP; Maris, JM; Gorlick, R; Kolb, EA; Lock, R; Carol, H; Keir, ST; Wu, J; Lyalin, D; Kurmasheva, RT; Houghton, PJ; Smith, MA

Published Date

  • August 2014

Published In

Volume / Issue

  • 61 / 8

Start / End Page

  • 1486 - 1489

PubMed ID

  • 24623675

Electronic International Standard Serial Number (EISSN)

  • 1545-5017

International Standard Serial Number (ISSN)

  • 1545-5009

Digital Object Identifier (DOI)

  • 10.1002/pbc.24989

Language

  • eng