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.
28435463
PMC5399591
10.7150/thno.18238
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."
Full citation
For attribution in academic contexts, please cite this work as:
Mikula, H., Stapleton, S., Kohler, R. H., Vinegoni, C., & Weissleder#, R. (2017). Design and Development of Fluorescent Vemurafenib Analogs for In Vivo Imaging. Theranostics, 7(5), 1257–1265. https://doi.org/10.7150/thno.18238
Mikula, H., Stapleton, S., Kohler, R. H., Vinegoni, C., & Weissleder#, R. (2017). Design and Development of Fluorescent Vemurafenib Analogs for In Vivo Imaging. Theranostics, 7(5), 1257–1265. https://doi.org/10.7150/thno.18238