PROTAC EGFR degrader 6

Names

[ CAS No. ]:
2409793-28-6

[ Name ]:
PROTAC EGFR degrader 6

Biological Activity

[Description]:

PROTAC EGFR degrader 6 (Compound 2), 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[1].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Signaling Pathways >> JAK/STAT Signaling >> EGFR
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR
Signaling Pathways >> PROTAC >> PROTAC

[Target]

IC50: 180 nM (EGFRDel19 in HCC827 cells)[1] DC50: 45.2 nM (EGFRDel19 in HCC827 cells)[1]


[In Vitro]

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 (Dmax = 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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C49H57FN12O5

[ Molecular Weight ]:
913.05


Related Compounds