PROTAC EGFR degrader 6 

PROTAC EGFR degrader 6, a PROTAC EGFR degrader, potently degrades EGFR^Del19 in HCC827 cells with the DC₅₀ of 45.2 nM. PROTAC EGFR degrader 6 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase^[1].

IC₅₀: 180 nM (EGFR^Del19 in HCC827 cells)^[1]
DC₅₀: 45.2 nM (EGFR^Del19 in HCC827 cells)^[1]

PROTAC EGFR degrader 6 (compound 2) (0.001-10 μM; 48 hours) exhibits potent EGFR degradation activity with certain concentration-dependent manner; and shows DC₅₀ of 45.2 nM in HCC827 cells^[1].
PROTAC EGFR degrader 6 (100 nM; 4-96 hours) degradates EGFR protein in a time-dependent manner, and reaches the maximum degradation rate (D_max = 87%) at 96 h^[1].
PROTAC EGFR degrader 6 (0.1, 1 and 10 μM; 48 hours) shows weak degradation activity on EGFR in H1975 and A549 cells^[1].
PROTAC EGFR degrader 6 (0.1 and 1 μM; 32 hours) induce HCC827 apoptosis, and the percentages of apoptosis cells are 53.72% and 32.31% at 0.1 and 1 μM, respectively^[1].

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

913.05

C₄₉H₅₇FN₁₂O₅

2409793-28-6

O=C1CCC(C(N1)=O)N2CC3=C(C2=O)C=CC=C3NC(CCCCCCCN4CCN(CC4)C5=CC=C(N=C5)NC6=NC=C7N=C(N=C(C7=C6)N8CCC(CC8)CO)NC9=CC=C(C=C9)F)=O

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• [1]. Hao Zhang, et al. Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC). Eur J Med Chem. 2020 Mar 1;189:112061.  [Content Brief]