PROTAC EGFR degrader 4
PROTAC EGFR degrader 4 is a potent PROTAC targeting mutant EGFR.PROTAC EGFR degrader 4 induces EGFRdel19 and EGFRL858R/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].
Product Specifications
CAS Number
[2882845-50-1]
UNSPSC
12352005
Target
Autophagy; EGFR; PROTACs
Type
Reference compound
Related Pathways
Autophagy; JAK/STAT Signaling; PROTAC; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/protac-egfr-degrader-4.html
Purity
99.70
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
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
Molecular Formula
C55H70N12O4S
Molecular Weight
995.29
References & Citations
[1]Hong-Yi Zhao, Discovery of potent small molecule PROTACs targeting mutant EGFR. Eur J Med Chem. 2020 Dec 15;208:112781.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, protect from light, stored under nitrogen)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Available Sizes
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