Potency assay (off target):
Linsitinib was tested against 88 kinases (Kinase Profiler, Upstate Inc) and 42 receptor tyrosine kinases (RTK, R&D systems). At 1 uM, none of the 88 kinases was inhibited >50%. In the RTK panel, 40 of the 42 kinases had IC50s >10 uM (INSR and INSRR, with IC50s ~75 nM, are listed as targets above).
Probe Selectivity in Vitro:
Negligible inhibition of CYP3A4, CYP2D6 and CYP1A2 (IC50 > 10 uM)