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 [1].
Product Specifications
CAS Number
2654821-05-1
UNSPSC
12352005
Target
EGFR; PROTACs
Related Pathways
JAK/STAT Signaling; PROTAC; Protein Tyrosine Kinase/RTK
Field of Research
Cancer
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
Molecular Formula
C48H48F2N10O6S
Molecular Weight
931.02
References & Citations
[1]NASVESCHUK Christopher, et al. Preparation of substituted 2- (6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-1-yl) -N-thiazol-2-yl-acetamides as EGFR degraders to treat cancer metastasis to the brain or CNS. World Intellectual Property Organization, WO2022251539 A2 2022-12-01.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
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