Lenvatinib, Free Base

Soluble in DMSO. Lenvatinib, also known as E7080, is an active inhibitor of multiple receptor tyrosine kinases, with IC50 values of 22 nM (VEGFR1), 4 nM (VEGFR2), 5.2 nM (VEGFR3), 46 nM (FGFR1), 51 nM (PDGFRa), 39 nM (PDGFRb), and 100 nM (KIT). It inhibited SCF- and VEGF-induced angiogenesis of human umbilical vein endothelial cells that express the SCF receptor KIT, with IC50 values of 5.2 nM and 5.1 nM, respectively. Lenvatinib inhibited tumor growth in the human small cell lung cancer H146 xenograft model. Matsui J., et al. 'E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition.' Int. J. Cancer 122: 664-671 (2008). This research compound is the free base form of lenvatinib. We also plan to offer the methanesulfonate salt form, please see Cat. No. L-5433, Lenvatinib, Methanesulfonate Salt. The methanesulfonate salt form will be added to our website as soon as the first lot is ready for shipment. The maximum tolerated dose (MTD) for lenvatinib with carboplatin/paclitaxel is 4?mg BID in advanced non-small cell lung cancer patients. Lenvatinib at the MTD demonstrated tolerability and encouraging antitumor activity. Nishio M., et al. 'Phase 1 study of lenvatinib combined with carboplatin and paclitaxel in patients with non-small-cell lung cancer.' Br. J. Cancer 109: 538-544 (2013). Lenvatinib had manageable toxicity and showed preliminary activity for durable disease control. The antiangiogenic activity of lenvatinib might be correlated with its antitumor activity in patients with a wide range of solid tumors. Yamada K., et al. 'Phase I dose-escalation study and biomarker analysis of E7080 in patients with advanced solid tumors.' Clin. Cancer Res. 17: 2528-2537 (2011).