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Foretinib

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Foretinib
Names
Preferred IUPAC name N-quinolin-4-yl}oxy)phenyl]-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
Other names XL880; EXEL-2880; GSK1363089; GSK089
Identifiers
CAS Number
3D model (JSmol)
ChEBI
ChEMBL
ChemSpider
DrugBank
ECHA InfoCard 100.158.129 Edit this at Wikidata
KEGG
PubChem CID
UNII
CompTox Dashboard (EPA)
InChI
  • Key: CXQHYVUVSFXTMY-UHFFFAOYSA-N
  • InChI=1S/C34H34F2N4O6/c1-43-30-20-25-27(21-31(30)45-16-2-13-40-14-17-44-18-15-40)37-12-9-28(25)46-29-8-7-24(19-26(29)36)39-33(42)34(10-11-34)32(41)38-23-5-3-22(35)4-6-23/h3-9,12,19-21H,2,10-11,13-18H2,1H3,(H,38,41)(H,39,42)
SMILES
  • COc1cc2c(ccnc2cc1OCCCN3CCOCC3)Oc4ccc(cc4F)NC(=O)C5(CC5)C(=O)Nc6ccc(cc6)F
Properties
Chemical formula C34H34F2N4O6
Molar mass 632.665 g·mol
Except where otherwise noted, data are given for materials in their standard state (at 25 °C , 100 kPa). Infobox references
Chemical compound

Foretinib is an experimental drug candidate for the treatment of cancer. It was discovered by Exelixis and is under development by GlaxoSmithKline. About 10 Phase II clinical trials have been run. As of October 2015 it appears development has been discontinued.

Foretinib is an inhibitor of the kinase enzymes c-Met and vascular endothelial growth factor receptor 2 (VEGFR-2).

See also

References

  1. Hedgethorne, K.; Huang, P.H. (2010). "Foretinib. c-Met and VEGFR-2 inhibitor, Oncolytic". Drugs of the Future. 35 (11): 893–901. doi:10.1358/dof.2010.35.11.1529012.
  2. "XL880 (GSK1363089)". Exelixis, Inc.
  3. "Foretinib". clinicaltrials.gov.
  4. "Foretinib - AdisInsight". adisinsight.springer.com. Retrieved 16 April 2018.
  5. Qian, F; Engst, S; Yamaguchi, K; Yu, P; Won, KA; Mock, L; Lou, T; Tan, J; et al. (2009). "Inhibition of tumor cell growth, invasion, and metastasis by EXEL-2880 (XL880, GSK1363089), a novel inhibitor of HGF and VEGF receptor tyrosine kinases". Cancer Research. 69 (20): 8009–16. doi:10.1158/0008-5472.CAN-08-4889. PMID 19808973.
Growth factor receptor modulators
Angiopoietin
CNTF
EGF (ErbB)
EGF
(ErbB1/HER1)
ErbB2/HER2
  • Agonists: Unknown/none
ErbB3/HER3
ErbB4/HER4
FGF
FGFR1
FGFR2
FGFR3
FGFR4
Unsorted
HGF (c-Met)
IGF
IGF-1
IGF-2
Others
LNGF (p75)
PDGF
RET (GFL)
GFRα1
GFRα2
GFRα3
GFRα4
Unsorted
SCF (c-Kit)
TGFβ
Trk
TrkA
  • Negative allosteric modulators: VM-902A
TrkB
TrkC
VEGF
Others
  • Additional growth factor receptor modulators: Cerebrolysin (neurotrophin mixture)
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