Foretinibfeatured
WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#:201372
CAS#:849217-64-7
Description:Foretinib, also known as XL880 and GSK1363089, is an orally bioavailable small molecule with potential antineoplastic activity. MET/VEGFR2 inhibitor GSK1363089 binds to and selectively inhibits hepatocyte growth factor (HGF) receptor c-MET and vascular endothelial growth factor receptor 2 (VEGFR2), which may result in the inhibition of tumor angiogenesis, tumor cell proliferation and metastasis. The proto-oncogene c-MET has been found to be over-expressed in a variety of cancers.
Price and Availability
Foretinib, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.
Chemical Structure
Theoretical Analysis
MedKoo Cat#: 201372Name: ForetinibCAS#: 849217-64-7Chemical Formula: C34H34F2N4O6Exact Mass: 632.24464Molecular Weight: 632.65377Elemental Analysis: C, 64.55; H, 5.42; F, 6.01; N, 8.86; O, 15.17
Synonym:XL880; XL 880; XL-880; GSK1363089; GSK 1363089; GSK-1363089; GSK089; EXEL2880; Foretinib.
IUPAC/Chemical Name:N-[3-fluoro-4-({6-methoxy-7-[3-(morpholin-4-yl)propoxy]quinolin-4-yl}oxy)phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
InChi Key:CXQHYVUVSFXTMY-UHFFFAOYSA-N
InChi Code: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 Code:O=C(C1(C(NC2=CC=C(F)C=C2)=O)CC1)NC3=CC=C(OC4=CC=NC5=CC(OCCCN6CCOCC6)=C(OC)C=C45)C(F)=C3
Technical Data
Additional Information
References
1: Bénard J. [ROS1 fusion proteins, targets offoretinib]. Bull Cancer. 2014 Jan 1;101(1):4. French. PubMed PMID:24649496.
2: Davare MA, Saborowski A, Eide CA, Tognon C, Smith RL, Elferich J,Agarwal A, Tyner JW, Shinde UP, Lowe SW, Druker BJ. Foretinib is apotent inhibitor of oncogenic ROS1 fusion proteins. Proc Natl Acad Sci US A. 2013 Nov 26;110(48):19519-24. doi: 10.1073/pnas.1319583110. Epub2013 Nov 11. PubMed PMID: 24218589; PubMed Central PMCID: PMC3845150.
3: Shah MA, Wainberg ZA, Catenacci DV, Hochster HS, Ford J, Kunz P, LeeFC, Kallender H, Cecchi F, Rabe DC, Keer H, Martin AM, Liu Y, Gagnon R,Bonate P, Liu L, Gilmer T, Bottaro DP. Phase II study evaluating 2dosing schedules of oral foretinib (GSK1363089), cMET/VEGFR2 inhibitor,in patients with metastatic gastric cancer. PLoS One. 2013;8(3):e54014.doi: 10.1371/journal.pone.0054014. Epub 2013 Mar 14. PubMed PMID:23516391; PubMed Central PMCID: PMC3597709.
4: Logan TF. Foretinib (XL880): c-MET inhibitor with activity inpapillary renal cell cancer. Curr Oncol Rep. 2013 Apr;15(2):83-90. doi:10.1007/s11912-013-0299-3. Review. PubMed PMID: 23408121.
5: Choueiri TK, Vaishampayan U, Rosenberg JE, Logan TF, Harzstark AL,Bukowski RM, Rini BI, Srinivas S, Stein MN, Adams LM, Ottesen LH,Laubscher KH, Sherman L, McDermott DF, Haas NB, Flaherty KT, Ross R,Eisenberg P, Meltzer PS, Merino MJ, Bottaro DP, Linehan WM, SrinivasanR. Phase II and biomarker study of the dual MET/VEGFR2 inhibitorforetinib in patients with papillary renal cell carcinoma. J Clin Oncol.2013 Jan 10;31(2):181-6. doi: 10.1200/JCO.2012.43.3383. Epub 2012 Dec 3.PubMed PMID: 23213094; PubMed Central PMCID: PMC3532390.
6: Shapiro GI, McCallum S, Adams LM, Sherman L, Weller S, Swann S, KeerH, Miles D, Müller T, Lorusso P. A Phase 1 dose-escalation study of thesafety and pharmacokinetics of once-daily oral foretinib, a multi-kinaseinhibitor, in patients with solid tumors. Invest New Drugs. 2013Jun;31(3):742-50. doi: 10.1007/s10637-012-9881-z. Epub 2012 Oct 6.PubMed PMID: 23054208.
7: Seiwert T, Sarantopoulos J, Kallender H, McCallum S, Keer HN,Blumenschein G Jr. Phase II trial of single-agent foretinib (GSK1363089)in patients with recurrent or metastatic squamous cell carcinoma of thehead and neck. Invest New Drugs. 2013 Apr;31(2):417-24. doi:10.1007/s10637-012-9861-3. Epub 2012 Aug 24. PubMed PMID: 22918720;PubMed Central PMCID: PMC3589657.
8: Huynh H, Ong R, Soo KC. Foretinib demonstrates anti-tumor activityand improves overall survival in preclinical models of hepatocellularcarcinoma. Angiogenesis. 2012 Mar;15(1):59-70. doi:10.1007/s10456-011-9243-z. Epub 2011 Dec 21. PubMed PMID: 22187171.
9: Dufies M, Jacquel A, Robert G, Cluzeau T, Puissant A, Fenouille N,Legros L, Raynaud S, Cassuto JP, Luciano F, Auberger P. Mechanism ofaction of the multikinase inhibitor Foretinib. Cell Cycle. 2011 Dec1;10(23):4138-48. doi: 10.4161/cc.10.23.18323. Epub 2011 Dec 1. PubMedPMID: 22101270.
10: Kataoka Y, Mukohara T, Tomioka H, Funakoshi Y, Kiyota N, Fujiwara Y,Yashiro M, Hirakawa K, Hirai M, Minami H. Foretinib (GSK1363089), amulti-kinase inhibitor of MET and VEGFRs, inhibits growth of gastriccancer cell lines by blocking inter-receptor tyrosine kinase networks.Invest New Drugs. 2012 Aug;30(4):1352-60. doi:10.1007/s10637-011-9699-0. Epub 2011 Jun 8. PubMed PMID: 21655918.
