Foretinib (GSK1363089)

Bezeichnung:Foretinib (GSK1363089)

CAS-Nr849217-64-7

Englisch Name:Foretinib (GSK1363089)

CBNumberCB02490083

SummenformelC34H34F2N4O6

Molgewicht632.65

MOL-Datei849217-64-7.mol

Foretinib (GSK1363089) physikalisch-chemischer Eigenschaften

Schmelzpunkt	>98°C (dec.)
Siedepunkt	828.5±65.0 °C(Predicted)
Dichte	1.372
storage temp.	Sealed in dry,Store in freezer, under -20°C
Löslichkeit	DMSO (Slightly), Ethanol (Slightly)
pka	13.14±0.70(Predicted)
Aggregatzustand	Yellow powder.
Farbe	Pale Yellow to Yellow
CAS Datenbank	849217-64-7

Gefahreninformationscode (GHS)

Foretinib (GSK1363089) Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Foretinib is a multikinase inhibitor that targets MET and VEGFR2 and also exhibits an inhibitory effect against KIT, Flt-3, PDGFRb, and Tie-2.
Verwenden
XL880 (GSK1363089, EXEL-2880) is an ATP-competitive inhibitor of MET and KDR with IC50 of 0.4 nM and 0.9 nM, respectively.
Verwenden
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
Einzelnachweise
[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) Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Send Inquriy