Abstract | BACKGROUND/AIM: MATERIALS AND METHODS: RESULTS: This drug showed treatment efficacy in naïve and imatinib-resistant BCR-ABL(+) leukemia cells, particularly in cells harboring T315I-mutated BCR-ABL, for which no effective inhibitor is available to date. By combination with the mTOR inhibitor RAD001, a synergistic effect on cell proliferation was observed in these cell lines. CONCLUSION:
TKI258 may become a potent therapeutic agent, either alone or in combination with RAD001, for treatment of BCR-ABL(+) leukemia.
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Authors | Jan Eucker, Chuanbing Zang, Yongan Zhou, Xinhua Li, Piet Habbel, Christian Neumann, Christian Scholz, Hongyu Liu |
Journal | Anticancer research
(Anticancer Res)
Vol. 34
Issue 9
Pg. 4909-14
(Sep 2014)
ISSN: 1791-7530 [Electronic] Greece |
PMID | 25202073
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Copyright | Copyright© 2014 International Institute of Anticancer Research (Dr. John G. Delinassios), All rights reserved. |
Chemical References |
- 4-amino-5-fluoro-3-(5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl)quinolin-2(1H)-one
- Antineoplastic Agents
- Benzimidazoles
- Protein Kinase Inhibitors
- Quinolones
- Everolimus
- Fusion Proteins, bcr-abl
- TOR Serine-Threonine Kinases
- Sirolimus
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Topics |
- Antineoplastic Agents
(pharmacology)
- Apoptosis
(drug effects)
- Benzimidazoles
(pharmacology)
- Cell Line, Tumor
- Cell Proliferation
(drug effects)
- Drug Synergism
- Everolimus
- Fusion Proteins, bcr-abl
(genetics)
- Humans
- Leukemia
(drug therapy, genetics)
- Protein Kinase Inhibitors
(pharmacology)
- Quinolones
(pharmacology)
- Sirolimus
(analogs & derivatives, pharmacology)
- TOR Serine-Threonine Kinases
(antagonists & inhibitors)
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