| Identification | Back Directory | [Name]
Foretinib (GSK1363089) | [CAS]
849217-64-7 | [Synonyms]
XL880
GSK089
Foretinib
EXEL-2880
GSK 1363089
EXEL-2880/XL-880
XL-880,Foretinib
Foretinib, >=98%
XL880(GSK1363089)
Foretinib (XL-880)
Foretinib, Free Base
GSK1363089/foretinib
Foretinib (GSK1363089)
Foretinib (GSK1363089, XL880)
N-(3-Fluoro-4-((6-methoxy-7-(3-morpholinopropoxy)quinolin-4-yl)-oxy)phenyl)-N-(4-fluorophenyl)
N-(3-Fluoro-4-((6-methoxy-7-(3-morpholinopropoxy)quinolin-4-yl)-oxy)phenyl)-N-(4-fluorophenyl)cyc
N-(3-fluoro-4-(6-Methoxy-7-(3-Morpholinopropoxy)quinolin-4-yloxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxaMide
N1'-[3-fluoro-4-[[6-Methoxy-7-(3-Morpholinopropoxy)-4-quinolyl]oxy]phenyl]-N1-(4-fluorophenyl)cyclopropane-1,1-dicarboxaMide
N-[3-Fluoro-4-[[6-(methyloxy)-7-[[3-(morpholin-4-yl)propyl]oxy]quinolin-4-yl]oxy]phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1
N-[3-Fluoro-4-[[6-methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinolinyl]oxy]phenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide
N-[3-Fluoro-4-[[6-(methyloxy)-7-[[3-(morpholin-4-yl)propyl]oxy]quinolin-4-yl]oxy]phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
foretinib
N1-{3-fluoro-4-[(6-(Methyloxy)-7-{[3-(4-Morpholinyl)propyl]oxy}-4-quinolinyl)oxy]phenyl}-N1'-(4-fluorophenyl)-1,1-cyclopropanedicarboxaMide | [Molecular Formula]
C34H34F2N4O6 | [MDL Number]
MFCD22379992 | [MOL File]
849217-64-7.mol | [Molecular Weight]
632.654 |
| Chemical Properties | Back Directory | [Melting point ]
>98°C (dec.) | [Boiling point ]
828.5±65.0 °C(Predicted) | [density ]
1.372 | [storage temp. ]
Sealed in dry,Store in freezer, under -20°C | [solubility ]
DMSO (Slightly), Ethanol (Slightly) | [form ]
Yellow powder. | [pka]
13.14±0.70(Predicted) | [color ]
Pale Yellow to Yellow | [CAS DataBase Reference]
849217-64-7 |
| Hazard Information | Back Directory | [Uses]
XL880 (GSK1363089, EXEL-2880) is an ATP-competitive inhibitor of MET and KDR with IC50 of 0.4 nM and 0.9 nM, respectively. | [Definition]
ChEBI:N1'-[3-fluoro-4-[[6-methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinolinyl]oxy]phenyl]-N1-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide is an aromatic ether. | [Clinical Use]
Foretinib has also shown to be effective against ROS1 mutations especially when acquired with crizotinib resistance. A clinical trial investigating the dosing and safety profile of combining foretinib and erlotinib was designed for advanced pretreated NSCLC patients. | [in vitro]
In vitro, foretinib blocks activation of MET and VEGFR2-induced signaling pathways. In vivo experiments show a dose-dependent decrease in tumor burden in a lung metastasis experimental model. | [target]
Met | [storage]
Store at -20°C | [References]
[1] qian f1, engst s, yamaguchi k, yu p, won ka, mock l, lou t, tan j, li c, tam d, lougheed j, yakes fm, bentzien f, xu w, zaks t, wooster r,greshock j, joly ah. inhibition of tumor cell growth, invasion, and metastasis by exel-2880 (xl880, gsk1363089), a novel inhibitor of hgf and vegf receptor tyrosine kinases. cancer res. 2009 oct 15;69(20):8009-16. doi: 10.1158/0008-5472.can-08-4889. |
| Questions And Answer | Back Directory | [Description]
Foretinib (GSK1363089) is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Less potent against Ron, Flt-1/3/4, Kit, PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2. |
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