Golvatinib (E7050)

Description: Golvatinib (formerly E-7050) is an orally bioavailable dual c-Met and VEGFR-2 inhibitor with potential antineoplastic activity. It inhibits c-Met and VEGFR-2 with IC50 of 14 nM and 16 nM, and shows no effects on bFGF-stimulated HUVEC growth (up to 1000 nM). Golvatinib shows potent anti-proliferative activity in vitro and high in vivo antitumor efficacy by binding to and inhibiting the activities of both c-Met and VEGFR-2, which are upregulated in various tumors and play important roles in tumor cell growth, migration and angiogenesis.

References: Cancer Sci. 2010; 101(1):210-5; Clin Cancer Res. 2012; 18(6):1663-71; Am J Pathol. 2012; 181(3):1034-43.

Synonym: E 7050; Golvatinib; E7050; E-7050;

IUPAC/Chemical Name: N-(2-fluoro-4-((2-(4-(4-methylpiperazin-1-yl)piperidine-1-carboxamido)pyridin-4-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1, 1-dicarboxamide

InChi Key: BWEYRDZIIMFBJR-UHFFFAOYSA-N

InChi Code: InChI=1S/C33H37F2N7O4/c1-39-16-18-40(19-17-39)23-9-14-41(15-10-23)32(45)38-29-21-26(8-13-37-29)46-25-6-7-28(27(35)20-25)42(24-4-2-22(34)3-5-24)31(44)33(11-12-33)30(36)43/h2-8, 13, 20-21, 23H, 9-12, 14-19H2, 1H3, (H2, 36, 43)(H, 37, 38, 45)

SMILES Code: O=C(C1(C(N)=O)CC1)N(C2=CC=C(OC3=CC(NC(N4CCC(N5CCN(C)CC5)CC4)=O)=NC=C3)C=C2F)C6=CC=C(F)C=C6