Publication: Design and Development of Fluorescent Vemurafenib Analogs for In Vivo Imaging
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Date
2017
Published Version
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Publisher
Ivyspring International Publisher
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Citation
Mikula, Hannes, Shawn Stapleton, Rainer H. Kohler, Claudio Vinegoni, and Ralph Weissleder. 2017. “Design and Development of Fluorescent Vemurafenib Analogs for In Vivo Imaging.” Theranostics 7 (5): 1257-1265. doi:10.7150/thno.18238. http://dx.doi.org/10.7150/thno.18238.
Research Data
Abstract
Herein we describe fluorescent derivatives of vemurafenib to probe therapeutic BRAF inhibition in live cells and in vivo. The compounds were evaluated and compared by determining target binding, inhibition of mutant BRAF melanoma cell lines and live cell imaging. We show that vemurafenib-BODIPY is a superior imaging drug to visualize the targets of vemurafenib in live cells and in vivo in non-resistant and resistant melanoma tumors.
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Keywords
fluorescence microscopy, imaging agents, kinase inhibitor, BRAF
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