From Wikipedia, the free encyclopedia
Foretinib
Names
Preferred IUPAC name
N 1 -[3-Fluoro-4-({6-methoxy-7-[3-(morpholin-4-yl)propoxy]quinolin-4-yl}oxy)phenyl]-N ′1 -(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
Other names
XL880; EXEL-2880; GSK1363089; GSK089
Identifiers
ChEBI
ChEMBL
ChemSpider
DrugBank
ECHA InfoCard
100.158.129
KEGG
UNII
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)
COc1cc2c(ccnc2cc1OCCCN3CCOCC3)Oc4ccc(cc4F)NC(=O)C5(CC5)C(=O)Nc6ccc(cc6)F
Properties
C 34 H 34 F 2 N 4 O 6
Molar mass
632.665 g·mol−1
Except where otherwise noted, data are given for materials in their
standard state (at 25 °C [77 °F], 100 kPa).
Chemical compound
Foretinib is an experimental drug candidate for the treatment of cancer.
[1] It was discovered by
Exelixis and is under development by
GlaxoSmithKline .
[2] About 10 Phase II clinical trials have been run.
[3] As of October 2015
[update] it appears development has been discontinued.
[4]
Foretinib is an
inhibitor of the kinase enzymes
c-Met and
vascular endothelial growth factor receptor 2 (VEGFR-2).
[5]
See also
References
^ 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 .
^
"XL880 (GSK1363089)" . Exelixis, Inc.
^
"Foretinib" . clinicaltrials.gov.
^
"Foretinib - AdisInsight" . adisinsight.springer.com . Retrieved 16 April 2018 .
^ 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 .
Angiopoietin
CNTF
EGF (ErbB)
FGF
FGFR1
FGFR2
Agonists:
Ersofermin
FGF (
1 ,
2 (bFGF) ,
3 ,
4 ,
5 ,
6 ,
7 (
KGF ),
8 ,
9 ,
10 (KGF2) ,
17 ,
18 ,
22 )
Palifermin
Repifermin
Selpercatinib
Sprifermin
Trafermin
FGFR3
FGFR4 Unsorted
HGF (c-Met)
IGF
LNGF (p75NTR )
PDGF
RET (GFL)
SCF (c-Kit)
TGFβ
Trk
TrkA
Negative allosteric modulators:
VM-902A
TrkB
Agonists:
3,7-DHF
3,7,8,2'-THF
4'-DMA-7,8-DHF
7,3'-DHF
7,8-DHF
7,8,2'-THF
7,8,3'-THF
Amitriptyline
BDNF
BNN-20
Deoxygedunin
Deprenyl
Diosmetin
DMAQ-B1
HIOC
LM22A-4
N-Acetylserotonin
NT-3
NT-4
Norwogonin (5,7,8-THF)
R7
R13
TDP6
TrkC
VEGF Others
Additional growth factors:
Adrenomedullin
Colony-stimulating factors (see
here instead)
Connective tissue growth factor (CTGF)
Ephrins (
A1 ,
A2 ,
A3 ,
A4 ,
A5 ,
B1 ,
B2 ,
B3 )
Erythropoietin (see
here instead)
Glucose-6-phosphate isomerase (GPI; PGI, PHI, AMF)
Glia maturation factor (GMF)
Hepatoma-derived growth factor (HDGF)
Interleukins /
T-cell growth factors (see
here instead)
Leukemia inhibitory factor (LIF)
Macrophage-stimulating protein (MSP; HLP, HGFLP)
Midkine (NEGF2)
Migration-stimulating factor (MSF; PRG4)
Oncomodulin
Pituitary adenylate cyclase-activating peptide (PACAP)
Pleiotrophin
Renalase
Thrombopoietin (see
here instead)
Wnt signaling proteins
Additional growth factor receptor modulators:
Cerebrolysin (neurotrophin mixture)