2654821-05-1
2654821-05-1
Chemical Structure
PROTAC EGFR degrader 12
- CAS 番号: 2654821-05-1
- Formula:C48H48F2N10O6S
- Molecular Weight:931.02
InChIKey: GCMGHESATZAFCJ-VKPZIYMTSA-N
SMILES: OC1(CCN(C2=C(C=C(C=C2)N[C@@H]3C(NC(CC3)=O)=O)F)CC1)CC(N4CC5(C4)CN(C6=CC=C(C7=CC(F)=C(CN(C8=O)C(C9=C%10N(CCC%10)C=N9)C(NC%11=NC=CS%11)=O)C8=C7)C=C6)C5)=O
Biological Activity: PROTAC EGFR degrader 12 (example 1) is a PROTAC degrader targeting EGFR that can effectively degrade EGFR mutants, but has little effect on EGFR WT. PROTAC EGFR degrader 12 shows IC50s against EGFRL858R-T790M (NCI-H1975 cells), EGFRL858R (NCI-H3255 cells), and EGFRL858R-T790M-L797S (NCI-H1975+CS cells) of all <50 nM[1].
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PROTAC EGFR degrader 12 | PROTAC EGFR degrader 12 (example 1) is a PROTAC degrader targeting EGFR that can effectively degrade EGFR mutants, but has little effect on EGFR WT. PROTAC EGFR degrader 12 shows IC50s against EGFRL858R-T790M (NCI-H1975 cells), EGFRL858R (NCI-H3255 cells), and EGFRL858R-T790M-L797S (NCI-H1975+CS cells) of all <50 nM. | |||||||||||||||||||||
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