Vorolanib, sunitinib, and axitinib: A comparative study of vascular endothelial growth factor receptor inhibitors and their anti-angiogenic effects
Fig 3
(A) IC50 curves for the three TKIs inhibiting VEGFR1, VEGFR2, and VEGFR3. (B) TIE2 IC50 curves for the three TKIs. The TIE2 IC50 confirmed the kinase screen data as the three tested TKIs differed greatly in their ability to inhibit TIE2 receptor. Note that all TKI compounds were prepared and tested in duplicate in a ten-dose IC50 model. (C) Computer modeling of axitinib with TIE2 receptor. On the left, the protein is displayed using ribbons while the protein surface is displayed using a white transparent pattern. The small molecule axitinib is shown as a teal stick image. The middle and left side of the figure shows the detailed analysis of the binding mode of small molecule simulation with TIE2 in a steady state. In the middle are 3D diagrams of interaction with the hydrogen bonds shown by a dotted line. On the right side is a 2D diagram depicting the axitinib interaction with hydrogen bonds indicated with a red arrow. IC50, half-maximal inhibitory concentration; TIE2, tyrosine kinase with immunoglobulin-like and EGF-like domains 2; TKI, tyrosine kinase inhibitor; VEGFR, vascular endothelial growth factor receptor.