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ZSH-2117

ZSH-2117 is a covalent and selective EGFR PROTAC degrader with a DC50 of 45 nM in Ba/F3-EGFRL858R/T790M/C797S cells. ZSH-2117 significantly inhibits cell proliferation and reduces the downstream EGFR signaling proteins level of AKT and ERK. ZSH-2117 effectively inhibits tumor growth in Ba/F3-EGFRL858R/T790M/C797S xenograft mice model[1]. Pink: EGFR ligand ; Blue: NEDD4 ligase ligand (HY-175159) ; Black: linker

Product Specifications

UNSPSC

12352005

Target

Akt; EGFR; ERK; PROTACs

Related Pathways

JAK/STAT Signaling; MAPK/ERK Pathway; PI3K/Akt/mTOR; PROTAC; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Field of Research

Cancer

Smiles

O=C(N1CCN(C2CCN(C3=CC=C(NC4=NC=C(Cl)C(NC5=CC=CC=C5P(C)(C)=O)=N4)C=C3Br)CC2)CC1)C6N=C6C7=CC=CC=C7

Molecular Formula

C36H39BrClN8O2P

Molecular Weight

762.08

References & Citations

[1]He X, et al. Covalent Recruitment of NEDD4 for Targeted Protein Degradation: Rational Design of Small Molecular Degraders. J Am Chem Soc. 2025 Jun 25;147 (25) :21512-21525.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Frequently Asked Questions

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