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Pediatr Blood Cancer. 2014 Aug;61(8):1486-9. doi: 10.1002/pbc.24989. Epub 2014 Feb 20.

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

Author information

1
Texas Tech University Health Sciences Center, Lubbock, Texas.

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 0.1 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.

KEYWORDS:

developmental therapeutics; mTOR inhibitor; preclinical testing

PMID:
24623675
PMCID:
PMC4248662
DOI:
10.1002/pbc.24989
[Indexed for MEDLINE]
Free PMC Article

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