| Products/Services Used | Details | Operation |
|---|---|---|
| Proteins, Expression, Isolation and Analysis | … Boiled 11 samples were loaded into bis-tris polyacrylamide gels (4–12%; Genscript, #M00654). Target proteins were transferred to nitrocellulose membranes which were probed with … | Get A Quote |
The EGFR C797S mutation is the most common on-target resistance mechanism to osimertinib in patients with advanced non-small cell lung cancer (NSCLC). Currently there are no effective treatment options for patients with NSCLC harboring EGFR C797S triple mutants (Del19/T790M/C797S and L858R/T790M/C797S). Herein, we report an orally bioavailable EGFR PROTAC, HJM-561, which selectively degrades the EGFR C797S-containing triple mutants. HJM-561 potently inhibits the proliferation of Del19/T790M/C797S and L858R/T790M/C797S Ba/F3 cells while sparing cells expressing wild-type EGFR. Oral administration of HJM-561 shows robust antitumor activity in EGFR Del19/T790M/C797S-driven Ba/F3 CDX and PDX models that were resist... More
