%0 Journal Article
%A Shreder, Kevin R.
%A Wong, Melissa S.
%A Nomanbhoy, Tyzoon
%A S. Leventhal, Phillip
%A Fuller, Stacy R.
%D 2004
%T Synthesis of AX7593, a
Quinazoline-Derived Photoaffinity Probe
for EGFR
%U https://acs.figshare.com/articles/journal_contribution/Synthesis_of_AX7593_a_Quinazoline_Derived_Photoaffinity_Probe_for_EGFR/3320950
%R 10.1021/ol048656a.s001
%2 https://acs.figshare.com/ndownloader/files/5159740
%K 280 nM
%K K b
%K tetraethyleneglycol linker
%K probe AX 7593. Photoaffinity
%K EGFR inhibitors PP 2
%K photoaffinity probe
%K AG
%K AX 7593
%X The synthesis of a photoaffinity probe for EGFR is described. O-Alkylation of 4-(meta-azidoanilino)-6-methoxy-7-hydroxy-quinazoline with a
protected tetraethyleneglycol linker followed by the attachment of tetramethylrhodamine yielded the fluorescent probe AX7593. Photoaffinity
labeling of EGFR by AX7593 (Kb = 280 nM) was shown to have an efficiency of 34% and to be competitive with the EGFR inhibitors PP2 and
AG1478.
%I ACS Publications