Defactinib (CAS: 1073154-85-4), also known as VS6063 and PF04554878, is an orally bioavailable, small-molecule focal adhesion kinase (FAK) inhibitor with potential antiangiogenic and antineoplastic activities. FAK inhibitor PF-04554878 inhibits FAK, which may prevent the integrin-mediated activation of several downstream signal transduction pathways, including ERK, JNK/MAPK and PI3K/Akt, thus inhibiting tumor cell migration, proliferation and survival. The tyrosine kinase FAK is, a signal transducer for integrins that is upregulated in many tumor cell types and is involved in tumor cell invasion, migration and proliferation.
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TGF-beta/Smad
VEGFR
