PROTAC EGFR degrader 4 

PROTAC EGFR degrader 4 is a potent PROTAC targeting mutant EGFR.PROTAC EGFR degrader 4 induces EGFR^del19 and EGFR^L858R/T790M degradation with DC₅₀s of 0.51 and 126 nM, respectively. PROTAC EGFR degrader 4 significantly inhibits growth of HCC827 and H1975 cell lines with IC₅₀s of 0.83 and 203.1 nM, respectively. Induced EGFR degradation is related to autophagy^[1].

PROTAC EGFR degrader 4 (compound P3) has antiproliferative activity against cancer cells A431 (EGFR WT), HCC827 (EGFR^del19) and H1975 (EGFR^L858R/T790M) with IC₅₀s of 245 ± 30 nM, 0.83 ± 0.30 nM and 203 ± 21 nM, respectively^[1].
PROTAC EGFR degrader 4 (0.3-100 nM; 48 hours) displays excellent activity of inducing EGFR^del19 degradation with a DC₅₀ values of 0.51 nM^[1].
PROTAC EGFR degrader 4 (3 and 100 nM; 48 hours) dramatically reduces the phosphorylation of EGFR and its downstream effector Akt in HCC827 and H1975 cell lines^[1].
PROTAC EGFR degrader 4 (10 and 100 nM; 48 hours) induces 31.07% and 44.80% of HCC827 cell line to undergo apoptosis at concentration of 10 and 100 nM, respectively; and arrests both HCC827 and H1975 cell lines at G1 phase^[1].

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

995.29

C₅₅H₇₀N₁₂O₄S

2882845-50-1

CC1=C(SC=N1)C2=CC=C(C=C2)CNC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)NC(CCCCCCN4CCN(CC4)C5=CC=C(C=C5)NC6=NC=C7N=C(N(C7=N6)C8CCCC8)NC9=CC=CC=C9)=O)=O)O)=O

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• [1]. Hong-Yi Zhao, Discovery of potent small molecule PROTACs targeting mutant EGFR. Eur J Med Chem. 2020 Dec 15;208:112781.  [Content Brief]