Initial testing (stage 1) of the investigational mTOR kinase inhibitor MLN0128 by the pediatric preclinical testing program.
Journal Article (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.
- 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
- August 2014
Volume / Issue
- 61 / 8
Start / End Page
- 1486 - 1489
Pubmed Central ID
Electronic International Standard Serial Number (EISSN)
Digital Object Identifier (DOI)
- United States