cas 20197-72-2, 6-AMINO-3,4-DIETHOXYBENZOIC ACID | Articles data ｜lookchem

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20197-72-2

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Anilinodialkoxyquinazolines: Screening epidermal growth factor receptor tyrosine kinase inhibitors for potential tumor imaging probes
The epidermal growth factor receptor (EGFR), a long-standing drug development target, is also a desirable target for imaging. Sixteen dialkoxyquinazoline analogues, suitable for labeling with positron-emitting isotopes, have been synthesized and evaluated in a battery of in vitro assays to ascertain their chemical and biological properties. These characteristics provided the basis for the adoption of a selection schema to identify lead molecules for labeling and in vivo evaluation. A new EGFR tyrosine kinase radiometric binding assay revealed that all of the compounds possessed suitable affinity (IC50 = 0.4-51 nM) for the EGFR tyrosine kinase. All of the analogues inhibited ligand-induced EGFR tyrosine phosphorylation (IC 50 = 0.8-20 nM). The HPLC-estimated octanol/water partition coefficients ranged from 2 to 5.5. Four compounds, 4-(2′-fluoroanilino)- and 4-(3′-fluoroanilino)-6,7-diethoxyquinazoline as well as 4-(3′-chloroanilino)- and 4-(3′-bromoanilino)-6,7- dimethoxyquinazoline, possess the best combination of characteristics that warrant radioisotope labeling and further evaluation in tumor-bearing mice.
VanBrocklin, Henry F.,Lim, John K.,Coffing, Stephanie L.,Hom, Darren L.,Negash, Kitaw,Ono, Michele Y.,Gilmore, Jennifer L.,Bryant, Ianthe,Riese II, David J.
p. 7445 - 7456
(2007/10/03)

Quinazoline derivatives and therapeutic use thereof
Quinazoline derivatives represented by the general formula pharmacologically acceptable salts thereof, and compositions containing such compounds are described. Methods for using the compounds for treatment of hyperproliferative disorders are also described.
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Page/Page column 18-19

(2008/06/13)

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Chemical Properties

Melting Point: 135-136℃ (decomposition) (ethanol )
Boiling Point: 379.8 °C at 760 mmHg
Flash Point:183.5 °C
Density: 1.215 g/cm³
PKA: 2.39±0.10(Predicted)
PSA: 81.78000
LogP: 2.34560

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