Drug Information

Drug General Information
Drug ID
D09ETH
Former ID
DIB016237
Drug Name
E-7050
Synonyms
C-Met and VEGF-2 tyrosine kinase inhibitor (oral, cancer), Eisai
Drug Type
Small molecular drug
Indication Head and neck cancer [ICD9: 140-149, 140-229; ICD10:C07-C14, C32-C33] Phase 1 [525301], [542872]
Company
Eisai Co Ltd
Structure
Download
2D MOL

3D MOL
Formula
C33H37F2N7O4
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
PubChem Compound ID
16118392
PubChem Substance ID
24765550, 28721555, 40652761, 141053681, 152258444, 160644595, 160647280, 162009761, 162011993, 162108794, 163312255, 164045124, 172918939, 174525694, 174531528, 185990484, 198990522, 223388544, 224233676, 225848215, 227908873, 247721050, 249565639, 249814484, 252160604, 252441725, 252451558, 252553660
Target and Pathway
Target(s) Vascular endothelial growth factor receptor 2 Target Info Modulator [530452]
Hepatocyte growth factor receptor Target Info Modulator [530452]
KEGG Pathway Ras signaling pathway
Rap1 signaling pathway
Cytokine-cytokine receptor interaction
Endocytosis
PI3K-Akt signaling pathway
VEGF signaling pathway
Focal adhesion
Proteoglycans in cancerhsa04014:Ras signaling pathway
Axon guidance
Adherens junction
Bacterial invasion of epithelial cells
Epithelial cell signaling in Helicobacter pylori infection
Malaria
Pathways in cancer
Transcriptional misregulation in cancer
Proteoglycans in cancer
MicroRNAs in cancer
Renal cell carcinoma
Melanoma
Central carbon metabolism in cancer
NetPath Pathway IL2 Signaling Pathway
PANTHER Pathway Angiogenesis
VEGF signaling pathway
Pathway Interaction Database HIF-2-alpha transcription factor network
Beta3 integrin cell surface interactions
Signaling events mediated by TCPTP
SHP2 signaling
S1P1 pathway
VEGF and VEGFR signaling network
Integrins in angiogenesis
Signaling events mediated by VEGFR1 and VEGFR2
Notch-mediated HES/HEY networkmet_pathway:Signaling events mediated by Hepatocyte Growth Factor Receptor (c-Met)
Arf6 signaling events
Posttranslational regulation of adherens junction stability and dissassembly
Direct p53 effectors
Syndecan-1-mediated signaling events
Stabilization and expansion of the E-cadherin adherens junction
a6b1 and a6b4 Integrin signaling
FGF signaling pathway
Regulation of retinoblastoma protein
Reactome Neurophilin interactions with VEGF and VEGFR
VEGF binds to VEGFR leading to receptor dimerization
Integrin cell surface interactions
EPHA-mediated growth cone collapse
VEGFA-VEGFR2 Pathway
VEGFR2 mediated cell proliferationR-HSA-416550:Sema4D mediated inhibition of cell attachment and migration
WikiPathways Focal Adhesion
Nifedipine Activity
Cardiac Progenitor Differentiation
Signaling by VEGF
AngiogenesisWP366:TGF beta Signaling Pathway
Signaling of Hepatocyte Growth Factor Receptor
Extracellular vesicle-mediated signaling in recipient cells
Signaling Pathways in Glioblastoma
miR-targeted genes in squamous cell - TarBase
miR-targeted genes in muscle cell - TarBase
miR-targeted genes in lymphocytes - TarBase
miR-targeted genes in epithelium - TarBase
Semaphorin interactions
References
Ref 525301ClinicalTrials.gov (NCT02533102) Pharmacokinetics and Food Effect of Single Oral Dose of E7050 in Healthy Volunteers.
Ref 542872(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7956).
Ref 530452E7050: a dual c-Met and VEGFR-2 tyrosine kinase inhibitor promotes tumor regression and prolongs survival in mouse xenograft models. Cancer Sci. 2010 Jan;101(1):210-5.

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