Novel VEGFR2 targeted inhibitors:screening and detection of anti-tumor biological properties

doi:10.3969/j.issn.1674-3806.2013.12.04

Abstract：Objective To screen effective medicine with VEGFR 2 inhibitory activity from 8 novel VEGFR2 targeted inhibitors and to determine their anti-tumor properties.Methods Two cell lines(Tca8113 cells from tongue cancer and HUVEC ) were cultured respectively in groups with 6 different concentrations of the eight inhibitors (marked No.1 to No.8).Positive control using different concentrations of 5-FU and blank control without medicine were set up simultaneously .Cell growth was measured by MTT assay .Immunocytochemistry was carried out to deter-mined VEGFR2 levels in groups with different saturated inhibitors or in blank control .Results Cell growths of both cell lines were significantly inhibited in positive control groups comparing to that in blank control ( P<0.05 );there was no significant difference in cell growth between VEGFR 2 inhibitor groups and blank control in the same cell line ( P>0.05 ) .Immunohistochemistry showed that VEGFR 2 was highly expressed on the cell membranes of Tca 8113 cells and HUVEC;comparing to blank control,only No.6 VEGFR2 targeted inhibitor decreased VEGFR2 expression on Tca8113 cells significantly ( P=0.000 ) , while all inhibitors showed no VEGFR 2 inhibition on either cell line ( P>0.05 ) .Conclusion These VEGFR2 targeted inhibitors have no proliferative inhibition on the cell lines of HUVEC and Tca8113.However, No.6 inhibitor decreases the VEGFR2 expression on Tca8113 cells significantly thus becom-ing a candidate for further study .