Foretinib
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Preferred IUPAC name N1-[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 | |
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ChEBI |
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DrugBank |
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ECHA InfoCard | 100.158.129 |
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InChI
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Properties | |
Chemical formula | C34H34F2N4O6 |
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). Infobox references |
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
- c-Met inhibitors
- Cabozantinib, a similar molecule and kinase inhibitor with FDA approval
- VEGFR inhibitor
- tyrosine-kinase inhibitor
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.
- v
- t
- e
- Agonists: Angiopoietin 1
- Angiopoietin 4
- Antagonists: Angiopoietin 2
- Angiopoietin 3
- Kinase inhibitors: Altiratinib
- CE-245677
- Rebastinib
- Antibodies: Evinacumab (against angiopoietin 3)
- Nesvacumab (against angiopoietin 2)
EGF (ErbB1/HER1) |
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ErbB2/HER2 |
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ErbB3/HER3 |
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ErbB4/HER4 |
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FGFR1 | |
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FGFR2 |
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FGFR3 | |
FGFR4 | |
Unsorted |
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- Agonists: Fosgonimeton
- Hepatocyte growth factor
- Potentiators: Dihexa (PNB-0408)
- Kinase inhibitors: Altiratinib
- AM7
- AMG-458
- Amuvatinib
- BMS-777607
- Cabozantinib
- Capmatinib
- Crizotinib
- Foretinib
- Golvatinib
- INCB28060
- JNJ-38877605
- K252a
- MK-2461
- PF-04217903
- PF-2341066
- PHA-665752
- SU-11274
- Tivantinib
- Volitinib
- Antibodies: Emibetuzumab
- Ficlatuzumab
- Flanvotumab
- Onartuzumab
- Rilotumumab
- Telisotuzumab
- Telisotuzumab vedotin
IGF-1 |
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IGF-2 |
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Others |
- Antagonists: ALE-0540
- Dexamethasone
- EVT-901 (SAR-127963)
- Testosterone
- Antibodies: Against NGF: ABT-110 (PG110)
- ASP-6294
- Fasinumab
- Frunevetmab
- Fulranumab
- MEDI-578
- Ranevetmab
- Tanezumab
- Aptamers: Against NGF: RBM-004
- Decoy receptors: LEVI-04 (p75NTR-Fc)
- Agonists: Becaplermin
- Platelet-derived growth factor (A, B, C, D)
- Kinase inhibitors: Agerafenib
- Avapritinib
- Axitinib
- Crenolanib
- Imatinib
- Lenvatinib
- Masitinib
- Motesanib
- Nintedanib
- Pazopanib
- Radotinib
- Quizartinib
- Ripretinib
- Sunitinib
- Sorafenib
- Toceranib
- Antibodies: Olaratumab
- Ramucirumab
- Tovetumab
GFRα1 |
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GFRα2 |
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GFRα3 |
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GFRα4 |
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Unsorted |
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- See here instead.
TrkA |
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TrkB |
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TrkC |
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- Agonists: Placental growth factor (PGF)
- Ripretinib
- Telbermin
- VEGF (A, B, C, D (FIGF))
- Allosteric modulators: Cyclotraxin B
- Kinase inhibitors: Agerafenib
- Altiratinib
- Axitinib
- Cabozantinib
- Cediranib
- Fruquintinib
- Lapatinib
- Lenvatinib
- Motesanib
- Nintedanib
- Pazopanib
- Pegaptanib
- Rebastinib
- Regorafenib
- Semaxanib
- Sorafenib
- Sunitinib
- Toceranib
- Tivozanib
- Vandetanib
- WHI-P 154
- Antibodies: Alacizumab pegol
- Bevacizumab
- Icrucumab
- Ramucirumab
- Ranibizumab
- Decoy receptors: Aflibercept
- 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)