Amuvatinib hydrochloride (MP470 hydrochloride)

Amuvatinib is a multi-targeted inhibitor of receptor tyrosine kinases that inhibits c-Kit, platelet-derived growth factor receptor α (PDGFRα), and c-Met (IC₅₀s = 10, 40, and 81 nM, respectively).¹ It inhibits growth and induces apoptosis in prostate cancer cell lines, with additive effects achieved when combined with erlotinib .¹ Amuvatinib sensitizes cancer cells to radiation and chemotherapeutic compounds, in part by inhibiting homologous recombination.^2,3,4

1.Qi, W., Cooke, L.S., Stejskal, A., et al.MP470, a novel receptor tyrosine kinase inhibitor, in combination with erlotinib inhibits the HER family/PI3K/Akt pathway and tumor growth in prostate cancerBMC Cancer9(142)1-12(2009) 2.Padda, S., Neal, J.W., and Wakelee, H.A.MET inhibitors in combination with other therapies in non-small cell lung cancerTransl. Lung Cancer Res.1(4)238-253(2012) 3.Welsh, J.W., Mahadevan, D., Ellsworth, R., et al.The c-Metreceptortyrosine kinaseinhibitor MP470 radiosensitizes glioblastomacellsRadiat. Oncol.4(69)(2009) 4.Zhao, H., Luoto, K.R., Meng, A.X., et al.The receptor tyrosine kinase inhibitor amuvatinib (MP470) sensitizes tumor cells to radio- and chemo-therapies in part by inhibiting homologous recombinationRadiother. Oncol.101(1)59-65(2011)