849217-64-7 Usage
Description
Foretinib (GSK1363089) is an ATP-competitive multikinase inhibitor that targets hepatocyte growth factor receptor (HGFR) and vascular endothelial growth factor receptor (VEGFR), with high specificity for Met and KDR, and moderate inhibitory effects against Ron, Flt-1/3/4, Kit, PDGFRα/β, and Tie-2. It is currently in Phase 2 of clinical development.
Uses
Used in Oncology:
Foretinib (GSK1363089) is used as an anticancer agent for targeting the proliferation and angiogenesis of cancer cells. It inhibits the activity of MET and VEGFR2, which are key drivers of tumor growth and blood vessel formation, leading to the suppression of tumor progression and metastasis.
Used in Drug Development:
Foretinib (GSK1363089) serves as a valuable compound in the development of targeted therapies for various cancers. Its multikinase inhibitory profile allows researchers to study its potential synergistic effects with other drugs and explore its efficacy in combination therapies for improved cancer treatment outcomes.
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.
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.
Check Digit Verification of cas no
The CAS Registry Mumber 849217-64-7 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,4,9,2,1 and 7 respectively; the second part has 2 digits, 6 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 849217-64:
(8*8)+(7*4)+(6*9)+(5*2)+(4*1)+(3*7)+(2*6)+(1*4)=197
197 % 10 = 7
So 849217-64-7 is a valid CAS Registry Number.
849217-64-7Relevant articles and documents
Preparation methods of tyrosine kinase inhibitor XJF007 and its intermediate
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, (2019/07/04)
The invention discloses preparation methods of tyrosine kinase inhibitor XJF007 with a general structural formula (I) and its intermediate. The preparation method of the tyrosine kinase inhibitor XJF007 employs a collecting synthesis strategy of construct
Preparation method of tyrosine enzyme inhibitor Foretinib
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, (2017/01/19)
The present invention provides a preparation method of a tyrosine enzyme inhibitor Foretinib. The method is as below: subjecting 1,1-cyclopropyl dicarboxylic acid diethyl ester to selective hydrolysis; amidating with p-fluoro aniline to obtain a compound shown in a formula 4; hydrolyzing and amidating with 4-amino-2-fluorophenol to obtain a compound shown in a formula 6; conducting substitution on 4-chloro-6-methoxy-7-quinolinol and N-(3-chloropropyl) morpholine to obtain a compound shown in formula 8; conducting substitution on the compound in formula 6 and compound shown in the formula 8 to obtain a target product N-[3-fluoro-4-({6-(methyl oxy)-7-[(3-morpholine-4-yl phenyl)-oxy] quinoline-4-yl}oxy)phenyl]-N'-(4-fluorophenyl) cyclopropane-1,1-dicarboamide crude product. The crude product is re-crystallized in an ethanol / acetone solution to obtain a high purity product with an overall yield of 44-55%. The method has the advantages of easy and feasible process, easily available raw materials, high overall yield and good product quality, and is applicable to industrial production.
METHODS OF PREPARING QUINOLINE DERIVATIVES
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Page/Page column 35-36, (2010/06/15)
A Method of preparing a compound of formula i(1) or a pharmaceutically acceptable salt thereof, wherein: R1 and R2 join together with the nitrogen atom to which they are attached form a 6 membered heterocycloalkyl X1 is H,