Synthesis of AX7593, a
Quinazoline-Derived Photoaffinity Probe
for EGFR
Kevin R. Shreder
Melissa S. Wong
Tyzoon Nomanbhoy
Phillip S. Leventhal
Stacy R. Fuller
10.1021/ol048656a.s001
https://acs.figshare.com/articles/journal_contribution/Synthesis_of_AX7593_a_Quinazoline_Derived_Photoaffinity_Probe_for_EGFR/3320950
The synthesis of a photoaffinity probe for EGFR is described. O-Alkylation of 4-(<i>meta</i>-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 <b>AX7593</b> (<i>K</i><sub>b</sub> = 280 nM) was shown to have an efficiency of 34% and to be competitive with the EGFR inhibitors PP2 and
AG1478.
2004-10-14 00:00:00
280 nM
K b
tetraethyleneglycol linker
probe AX 7593. Photoaffinity
EGFR inhibitors PP 2
photoaffinity probe
AG
AX 7593