PF573,228 is a compound that targets focal adhesion kinase
(FAK), a non-receptor protein kinase, which is over-expressed
in various tumors. The aim of this study was to
evaluate the effects of PF573,228 on the cells derived from
mouse vascular tumors, namely, endothelioma cells.
The treatment of endothelioma cells with PF573,228 reduced
their growth with an IC50 of approximately 4.6 μmol L–1 and
inhibited cell migration with an IC50 of about 0.01 μmol L–1.
Microscopic studies revealed morphological attributes of
apoptosis. These observations were confirmed by ELISA,
which showed increased caspase-3 activity. PF573,228 also
inhibited angiogenesis in a dose-dependent manner, with
an IC50 of approximately 3.7 μmol L–1, and abrogated the
phosphorylation of cell survival proteins, proline-rich Akt
substrate (PRAS40) and S6 ribosomal protein (S6RP). Array
data further revealed that PF573,228 induced caspase-3 activation,
thus promoting apoptosis. Since all the processes
inhibited by PF573,228 provide important support to tumor
survival and progression, the drug may have a potential
role in the treatment of vascular tumors.