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. Author manuscript; available in PMC: 2015 Jun 16.
Published in final edited form as: Chembiochem. 2014 May 14;15(9):1317–1324. doi: 10.1002/cbic.201402010

Figure 2. Cellular activity of dasatinib-BODIPY.

Figure 2

Inhibition of the proliferation of BCR-Abl Ba/F3 cells was used as a proxy to demonstrate cell penetrance as well as recognition and inhibition of BCR-Abl. Cell viability was measured in the presence of increasing concentrations of dasatinib, dasatinib-BODIPY, and free BODIPY to permit determination of IC50 values. Despite a 23-fold decrease in potency relative to dasatinib, dasatinib-BODIPY was a potent, sub-micromolar inhibitor of BCR-Abl Ba/F3 cell proliferation. This was due to the kinase-targeting moiety of dasatinib-BODIPY since free BOIDPY had no detectable effect on the viability of these cells.