10.1021/ol048656a.s001
Kevin R. Shreder
Kevin R.
Shreder
Melissa S. Wong
Melissa S.
Wong
Tyzoon Nomanbhoy
Tyzoon
Nomanbhoy
Phillip S. Leventhal
Phillip
S. Leventhal
Stacy R. Fuller
Stacy R.
Fuller
Synthesis of AX7593, a
Quinazoline-Derived Photoaffinity Probe
for EGFR
American Chemical Society
2004
280 nM
K b
tetraethyleneglycol linker
probe AX 7593. Photoaffinity
EGFR inhibitors PP 2
photoaffinity probe
AG
AX 7593
2004-10-14 00:00:00
Journal contribution
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.