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编 号:F752165
分子式:C49H57FN12O5
分子量:913.05
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PROTAC EGFR degrader 6, a PROTAC EGFR degrader, potently degrades EGFRDel19 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.

体外研究:
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.PROTAC EGFR degrader 6 (100 nM; 4-96 hours) degradates EGFR protein in a time-dependent manner, and reaches the maximum degradation rate (Dmax = 87%) at 96 h.PROTAC EGFR degrader 6 (0.1, 1 and 10 μM; 48 hours) shows weak degradation activity on EGFR in H1975 and A549 cells.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.
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