Initial testing (stage 1) of the investigational mTOR kinase inhibitor MLN0128 by the pediatric preclinical testing program.
Publication
, Journal Article
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 in: Pediatr Blood Cancer
August 2014
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.
Duke Scholars
Altmetric Attention Stats
Dimensions Citation Stats
Published In
Pediatr Blood Cancer
DOI
EISSN
1545-5017
Publication Date
August 2014
Volume
61
Issue
8
Start / End Page
1486 / 1489
Location
United States
Related Subject Headings
- Xenograft Model Antitumor Assays
- TOR Serine-Threonine Kinases
- Pyrimidines
- Protein Kinase Inhibitors
- Oncology & Carcinogenesis
- Neoplasms, Experimental
- Neoplasm Proteins
- Mice
- Dose-Response Relationship, Drug
- Cell Line, Tumor
Citation
APA
Chicago
ICMJE
MLA
NLM
Kang, M. H., Reynolds, C. P., Maris, J. M., Gorlick, R., Kolb, E. A., Lock, R., … Smith, M. A. (2014). Initial testing (stage 1) of the investigational mTOR kinase inhibitor MLN0128 by the pediatric preclinical testing program. Pediatr Blood Cancer, 61(8), 1486–1489. https://doi.org/10.1002/pbc.24989
Kang, Min H., C Patrick Reynolds, John M. Maris, Richard Gorlick, E Anders Kolb, Richard Lock, Hernan Carol, et al. “Initial testing (stage 1) of the investigational mTOR kinase inhibitor MLN0128 by the pediatric preclinical testing program.” Pediatr Blood Cancer 61, no. 8 (August 2014): 1486–89. https://doi.org/10.1002/pbc.24989.
Kang MH, Reynolds CP, Maris JM, Gorlick R, Kolb EA, Lock R, et al. Initial testing (stage 1) of the investigational mTOR kinase inhibitor MLN0128 by the pediatric preclinical testing program. Pediatr Blood Cancer. 2014 Aug;61(8):1486–9.
Kang, Min H., et al. “Initial testing (stage 1) of the investigational mTOR kinase inhibitor MLN0128 by the pediatric preclinical testing program.” Pediatr Blood Cancer, vol. 61, no. 8, Aug. 2014, pp. 1486–89. Pubmed, doi:10.1002/pbc.24989.
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. Initial testing (stage 1) of the investigational mTOR kinase inhibitor MLN0128 by the pediatric preclinical testing program. Pediatr Blood Cancer. 2014 Aug;61(8):1486–1489.
Published In
Pediatr Blood Cancer
DOI
EISSN
1545-5017
Publication Date
August 2014
Volume
61
Issue
8
Start / End Page
1486 / 1489
Location
United States
Related Subject Headings
- Xenograft Model Antitumor Assays
- TOR Serine-Threonine Kinases
- Pyrimidines
- Protein Kinase Inhibitors
- Oncology & Carcinogenesis
- Neoplasms, Experimental
- Neoplasm Proteins
- Mice
- Dose-Response Relationship, Drug
- Cell Line, Tumor