golvatinib   Click here for help

GtoPdb Ligand ID: 7956

Synonyms: E-7050 | E7050
PDB Ligand
Compound class: Synthetic organic
Comment: Golvatinib is an orally bioavailable dual kinase inhibitor of c-Met (hepatocyte growth factor receptor) and VEGFR2 (vascular endothelial growth factor receptor-2) tyrosine kinases with potential antineoplastic activity [1]. It is the first kinase inhibitor with this dual action.
Click here for help
2D Structure
Click here for help
Click here for structure editor
Physico-chemical Properties
Click here for help
Hydrogen bond acceptors 10
Hydrogen bond donors 3
Rotatable bonds 12
Topological polar surface area 119.14
Molecular weight 633.29
XLogP 3.63
No. Lipinski's rules broken 0
Click here for help
Canonical SMILES CN1CCN(CC1)C1CCN(CC1)C(=O)Nc1nccc(c1)Oc1ccc(c(c1)F)NC(=O)C1(CC1)C(=O)Nc1ccc(cc1)F
Isomeric SMILES CN1CCN(CC1)C1CCN(CC1)C(=O)Nc1nccc(c1)Oc1ccc(c(c1)F)NC(=O)C1(CC1)C(=O)Nc1ccc(cc1)F
InChI InChI=1S/C33H37F2N7O4/c1-40-16-18-41(19-17-40)24-9-14-42(15-10-24)32(45)39-29-21-26(8-13-36-29)46-25-6-7-28(27(35)20-25)38-31(44)33(11-12-33)30(43)37-23-4-2-22(34)3-5-23/h2-8,13,20-21,24H,9-12,14-19H2,1H3,(H,37,43)(H,38,44)(H,36,39,45)
No information available.
Summary of Clinical Use Click here for help
Phase 2 clinical trials assessing golvatinib in combination with other antineoplastics, for various types of solid tumours have been completed. Click here to link to ClinicalTrials.gov's full list of golvatinib (as E7050) trials.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
The HGF/c-Met signalling pathway contributes to tumour proliferation, survival, migration, and infiltration in various types of cancer. The VEGF-induced activation of VEGFR2 induces proliferation and migration in endothelial cells and promotes angiogenesis, a crucial mechanism required to support tumour growth. It is proposed that by inhibiting both the c-Met and VEGFR2 pathways concommitantly, golvatinib should have more effective antitumour activity than compounds that inhibit only a single pathway [1].