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Golvatinib
- E 7050
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C33H37F2N7O4
- MW: 633.69
Description
Golvatinib (E7050) is an orally available dual c-MET/HGFR and VEGFR2 inhibitor with reported IC50 values of 14 nM for c-MET and 16 nM for VEGFR2. It inhibits receptor tyrosine kinase signaling involved in tumor growth and angiogenesis.
MET signaling drives tumor cell proliferation, survival, invasion and resistance mechanisms, while VEGFR2 controls vascular endothelial responses. Golvatinib is useful for studying combined tumor-intrinsic MET blockade and antiangiogenic VEGFR2 inhibition.
Key Features
- Dual c-MET and VEGFR2 inhibitor
- Reported IC50: 14 nM (c-MET) and 16 nM (VEGFR2)
- Targets tumor growth, survival and vascular signaling pathways
- Relevant to receptor tyrosine kinase oncology models
Applications
- MET/HGFR signaling studies
- Angiogenesis assays
- Tumor invasion and survival models
- RTK inhibitor profiling
More Information
| Parent CAS No. | 928037-13-2 |
|---|---|
| Chemical Name | N-(2-fluoro-4-(2-(4-(4-methylpiperazin-1-yl)piperidine-1-carboxamido)pyridin-4-yloxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide |
| SMILES | C1(C(NC2=CC=C(F)C=C2)=O)(C(NC2=CC=C(OC3C=CN=C(NC(N4CCC(N5CCN(C)CC5)CC4)=O)C=3)C=C2F)=O)CC1 |
| MFCD | MFCD22124462 |
| 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) |
| InChiKey | UQRCJCNVNUFYDX-UHFFFAOYSA-N |
| CID | 16118392 |
| Short Description | MET/VEGFR2 inhibitor |
References
- T Nakagawa et al. E7050: A dual c-Met and VEGFR-2 tyrosine kinase inhibitor promotes tumor regression and prolongs survival in mouse xenograft models. Cancer Science 2010, 101(1), 210-215.
- W Wang et al. Met kinase inhibitor E7050 reverses three different mechanisms of hepatocyte growth factor-induced tyrosine kinase inhibitor resistance in EGFR mutant lung cancer. Clin Cancer Res. 2012, 18(6):1663-1671.
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