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Theranostics 2017; 7(5):1257-1265. doi:10.7150/thno.18238 This issue Cite

Research Paper

Design and Development of Fluorescent Vemurafenib Analogs for In Vivo Imaging

Hannes Mikula^1*, Shawn Stapleton^1*, Rainer H. Kohler¹, Claudio Vinegoni¹, Ralph Weissleder^{1, 2✉}

1. Center for Systems Biology, Massachusetts General Hospital, 185 Cambridge Street, CPZN 5206, Boston, MA, 02114, USA;
2. Department of Systems Biology, Harvard Medical School, 200 Longwood Ave, Boston, MA, 02115, USA.
* These authors contributed equally

✉ Corresponding author: Prof. Ralph Weissleder, E-mail: rweisslederharvard.edu

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.

Keywords: fluorescence microscopy, imaging agents, kinase inhibitor, BRAF

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