PROTAC EGFR degrader 12 - CAS 2654821-05-1

PROTACEGFRdegrader 12 (example 1) is a PROTAC degrader that selectively targets and degrades mutant EGFR, with minimal effect on EGFRWT. It demonstrates an IC50 of less than 50 nM against EGFRL858R-T790M (NCI-H1975 cells), EGFRL858R (NCI-H3255 cells), and EGFRL858R-T790M-L797S (NCI-H1975+CS cells) .

EGFR, PROTACs

JAK/STAT signaling, Tyrosine Kinase/Adaptors, PROTAC, Angiogenesis

2654821-05-1

C48H48F2N10O6S

931.02

C(CC1(O)CCN(CC1)C2=C(F)C=C(N[C@@H]3C(=O)NC(=O)CC3)C=C2)(=O)N4CC5(CN(C5)C6=CC=C(C=C6)C=7C=C8C(=C(F)C7)CN(C(C(NC9=NC=CS9)=O)C%10=C%11N(C=N%10)CCC%11)C8=O)C4

-20°C

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PROTAC