Foretinib (GSK1363089)
Foretinib (GSK1363089) Basic information
- Product Name:
- Foretinib (GSK1363089)
- Synonyms:
-
- Foretinib
- GSK 1363089
- EXEL-2880
- XL880
- 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
- N-[3-Fluoro-4-[[6-methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinolinyl]oxy]phenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide
- XL-880,Foretinib
- XL880(GSK1363089)
- CAS:
- 849217-64-7
- MF:
- C34H34F2N4O6
- MW:
- 632.65
- Product Categories:
-
- Inhibitors
- Mol File:
- 849217-64-7.mol
Foretinib (GSK1363089) Chemical Properties
- 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)
- pka
- 13.14±0.70(Predicted)
- form
- Yellow powder.
- color
- Pale Yellow to Yellow
- CAS DataBase Reference
- 849217-64-7
Foretinib (GSK1363089) Usage And Synthesis
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.
Description
Foretinib is a multikinase inhibitor that targets MET and VEGFR2 and also exhibits an inhibitory effect against KIT, Flt-3, PDGFRb, and Tie-2.
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.
Uses
Foretinib (GSK1363089) is an ATP-competitive inhibitor of hepatocyte growth factor (HGF) and Vascular endothelial growth factor (VEGF) Receptor Tyrosine Kinases.
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
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.
Foretinib (GSK1363089)Supplier
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CAS:849217-64-7
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- Product Name:Foretinib (GSK1363089)
CAS:849217-64-7
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- Product Name:N-[3-Fluoro-4-[[6-methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinolinyl]oxy]phenyl]-N-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide
CAS:849217-64-7
Purity:98% HPLC Package:50mg;100mg;500mg;1g;5g;10g Remarks:Biochemical Reagents; Pharmaceutical Intermediates
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- Product Name:XL-880 ; Foretinib
CAS:849217-64-7
Purity:98% HPLC Package:50.0mg;100.0mg; 200.0mg;500mg;1g;5g; 10g
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- Products Intro
- Product Name:Foretinib, Free Base
CAS:849217-64-7
Purity:99+% Package:5Mg;25Mg;50Mg;100Mg;250Mg;500Mg