“…The PKs have been selected for the determination of an IC 50 profile of 1 because they are involved in malignant diseases and because they represent different PK families. As can be seen in Table , 1 is actually selective over the homologous TKs including EGF-R, ERbB2, TIE2, PDGFRβ, SRC, and FAK. , Compound 1 inhibited VEGF-R2/3 in the low nanomolar range, but compared to VEGF-R2, the kinases PDGFRβ inhibited in an almost 300-fold higher concentration (IC 50 = 6.8 × 10 -7 M), FAK (IC 50 = 9.7 × 10 -7 M) and the other PKs (EPHB4, IGF1-R, ABL1, INS-R, PLK1, CDK2/4, GSK3-β, NEK2, Aurora A/B 41 ) in only the micromolar range. In particular, the selectivity of 1 for VEGF-R2/3 over INS-R is important because a critical requirement for a PK inhibitor to be further developed is to avoid disturbing glucose homeostasis .…”