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Mol Cancer Ther. 2011 Sep;10(9):1542-52. doi: 10.1158/1535-7163.MCT-11-0426. Epub 2011 Jul 15.

Potent, selective inhibitors of fibroblast growth factor receptor define fibroblast growth factor dependence in preclinical cancer models.

Author information

1
Novartis Pharma AG, Basel, Switzerland.

Abstract

We describe here the identification and characterization of 2 novel inhibitors of the fibroblast growth factor receptor (FGFR) family of receptor tyrosine kinases. The compounds exhibit selective inhibition of FGFR over the closely related VEGFR2 receptor in cell lines and in vivo. The pharmacologic profile of these inhibitors was defined using a panel of human tumor cell lines characterized for specific mutations, amplifications, or translocations known to activate one of the four FGFR receptor isoforms. This pharmacology defines a profile for inhibitors that are likely to be of use in clinical settings in disease types where FGFR is shown to play an important role.

PMID:
21764904
DOI:
10.1158/1535-7163.MCT-11-0426
[Indexed for MEDLINE]
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