Extended Data Fig. 9: FK-Lapatinib is a FKBP12-dependent EGFR/HER2 kinase inhibitor. | Nature

Extended Data Fig. 9: FK-Lapatinib is a FKBP12-dependent EGFR/HER2 kinase inhibitor.

From: Brain-restricted mTOR inhibition with binary pharmacology

Extended Data Fig. 9

a, Chemical structures of Lapatinib and FK-Lapatinib. b, Inhibition of EGFR and HER2 kinase activity by Lapatinib and FK-Lapatinib in the absence or presence of supplemented 10 µM recombinant FKBP12 protein (n = 2, data are presented as individual points). c, Inhibition of proliferation of SK-BR3 cells by lapatinib and FK-lapatinib in the presence of absence of 10 µM RapaBlock (n = 3, data are presented as mean values +/− SD). d, SK-BR3 cells were treated with Lapatinib, FK-Lapatinib, and/or RapaBlock for 1 h and analyzed by immunoblot. Results shown are representative of three independent experiments. GAPDH is a sample processing control. For gel source data, see Supplementary Fig. 1.

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