PROTAC EGFR degrader 6

PROTAC EGFR degrader 6 (compound 2) shows greater antiproliferative potency against HCC827 (EGFR^Del19) cells than against H1975, A549, and A431 cells^[1].
PROTAC EGFR degrader 6 (1-10000 nM; 48 h) potently induces concentration-dependent degradation of EGFR in HCC827 (EGFR^Del19) cells with a DC₅₀ of 45.2 nM^[1].
PROTAC EGFR degrader 6 (100 nM; 4-96 h) induces time-dependent degradation of EGFR in HCC827 (EGFR^Del19) cells, reaching a maximum degradation rate of 87% at 96 h^[1].
PROTAC EGFR degrader 6 (0.1-1 μM; 36 h) inhibits EGFR and downstream Akt phosphorylation in a concentration-dependent manner in HCC827 (EGFR^Del19) cells, with potency comparable to reference EGFR inhibitors^[1].
PROTAC EGFR degrader 6 (0.1 μM; 32 h, preceded by 1 μM EGFR inhibitor 1 for 6 h) relies on EGFR binding for its degradation activity in HCC827 (EGFR^Del19) cells, as shown by reduced activity following pretreatment with EGFR inhibitor 1^[1].
PROTAC EGFR degrader 6 (0.1-10 μM; 48 h) shows weak EGFR degradation activity in H1975 (EGFR^L858R/T790M) and A549 (EGFR^WT) cells compared to its activity in HCC827 (EGFR^Del19) cells^[1].
PROTAC EGFR degrader 6 (0.1-1 μM; 32 h) induces concentration-dependent apoptosis in HCC827 (EGFR^Del19) cells, with 32.31% apoptotic cells at 0.1 μM and 53.72% apoptotic cells at 1 μM after 32 h^[1].
PROTAC EGFR degrader 6 (0.1-1 μM; 32 h) arrests HCC827 (EGFR^Del19) cells in the G1 phase, with 82.95% of cells in G1 at 0.1 μM and 81.89% of cells in G1 at 1 μM after 32 h^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.