Golvatinib - CAS 928037-13-2
Catalog number: 928037-13-2
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
golvatinib (also known as E7050) is an orally bioavailable dual kinase inhibitor of c-Met (hepatocyte growth factor receptor) and VEGFR-2 (vascular endothelial growth factor receptor-2) tyrosine kinases with potential antineoplastic activity. c-Met/VEGFR kinase inhibitor E7050 binds to and inhibits the activities of both c-Met and VEGFR-2, which may inhibit tumor cell growth and survival of tumor cells that overexpress these receptor tyrosine kinases. c-Met and VEGFR-2 are upregulated in a variety of various tumor cell types and play important roles in tumor cell growth, migration and angiogenesis.
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white solid powder
E7050; E-7050; E 7050; Golvatinib.
Current Developer:
Eisai Inc.
1.A phase I, dose-escalation study of the multitargeted receptor tyrosine kinase inhibitor, golvatinib, in patients with advanced solid tumors.
Molife LR1, Dean EJ2, Blanco-Codesido M3, Krebs MG2, Brunetto AT3, Greystoke AP2, Daniele G3, Lee L4, Kuznetsov G5, Myint KT5, Wood K6, de Las Heras B6, Ranson MR2. Clin Cancer Res. 2014 Dec 15;20(24):6284-94. doi: 10.1158/1078-0432.CCR-14-0409. Epub 2014 Oct 2.
PURPOSE: Receptor tyrosine kinases c-Met and Ron transduce signals regulating cell migration and matrix invasion. This phase I dose-escalation trial tested golvatinib, a highly potent, small-molecule, ATP-competitive inhibitor of c-Met and multiple members of the Eph receptor family plus c-Kit and Ron.
2.Multitargeting strategy using lenvatinib and golvatinib: maximizing anti-angiogenesis activity in a preclinical cancer model.
Nakazawa Y1, Kawano S, Matsui J, Funahashi Y, Tohyama O, Muto H, Nakagawa T, Matsushima T. Cancer Sci. 2015 Feb;106(2):201-7. doi: 10.1111/cas.12581. Epub 2015 Feb 4.
Almost all cancers show intrinsic and/or evasive resistance to vascular endothelial growth factor (VEGF) inhibitors by multiple mechanisms. Serum angiopoietin-2 (Ang2) level has been proposed as a potential biomarker of VEGF inhibitor response in several cancers. From these clinical observations, the Ang2 and Tie2 (its receptor) axis has been focused on as a promising target. Here, we show a novel strategy to circumvent the resistance by combining multi-tyrosine kinase inhibitors lenvatinib (VEGF receptor, fibroblast growth factor receptor, and RET inhibitor) and golvatinib (E7050; c-Met, Tie2, and EphB4 inhibitor). Tie2 identifies a highly pro-angiogenic macrophage subset, Tie2-expressing macrophages (TEM). Angi-Tie2 and EphB4-EphrinB2 signaling plays critical roles in pericyte-mediated vessel stabilization. In vitro analyses suggested that golvatinib combined with lenvatinib inhibited pericyte-mediated vessel stabilization and TEM differentiation.
3.Lenvatinib in combination with golvatinib overcomes hepatocyte growth factor pathway-induced resistance to vascular endothelial growth factor receptor inhibitor.
Nakagawa T1, Matsushima T, Kawano S, Nakazawa Y, Kato Y, Adachi Y, Abe T, Semba T, Yokoi A, Matsui J, Tsuruoka A, Funahashi Y. Cancer Sci. 2014 Jun;105(6):723-30. doi: 10.1111/cas.12409. Epub 2014 Apr 28.
Vascular endothelial growth factor receptor (VEGFR) inhibitors are approved for the treatment of several tumor types; however, some tumors show intrinsic resistance to VEGFR inhibitors, and some patients develop acquired resistance to these inhibitors. Therefore, a strategy to overcome VEGFR inhibitor resistance is urgently required. Recent reports suggest that activation of the hepatocyte growth factor (HGF) pathway through its cognate receptor, Met, contributes to VEGFR inhibitor resistance. Here, we explored the effect of the HGF/Met signaling pathway and its inhibitors on resistance to lenvatinib, a VEGFR inhibitor. In in vitro experiments, addition of VEGF plus HGF enhanced cell growth and tube formation of HUVECs when compared with stimulation by either factor alone. Lenvatinib potently inhibited the growth of HUVECs induced by VEGF alone, but cells induced by VEGF plus HGF showed lenvatinib resistance. This HGF-induced resistance was cancelled when the Met inhibitor, golvatinib, was added with lenvatinib.
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