Foretinib (GSK1363089) is a potent multi-kinase inhibitor of HGFR, VEGFR, KIT, Flt, PDGFR and Tie-2. In a cell-free assay, Foretinib (GSK1363089) is most potent for Met, KDR, and Tie-2, with IC50 values of 0.4 nM, 0.86 nM, and 1.1 nM, respectively. Foretinib (GSK1363089) also inhibits Ron, Flt1/3/4, KIT, and PDGFR?/?, with higher IC50 values ranging from 3 nM to 9.6 nM. [1] It binds tightly to Met and KDR with a very slow off-rate and inhibits tumor formation in an in vivo murine model of lung metastasis. [1]
A recent report showed that Foretinib (GSK1363089), by targeting cMet, significantly reduced primary medulloblastoma growth and invasion, and increased survival in disseminated mouse models of sonic hedgehog (SHH)-driven medulloblastoma. [2]
Foretinib (GSK1363089) has been examined in multiple clinical trials in wild-range of cancer patients including metastatic breast cancer, metastatic gastric cancer, papillary renal cell carcinoma (PRC), liver cancer, non-small-cell lung cancer, and squamous cell cancer of the head and neck."