PROTAC EGFR degrader 14

PROTAC EGFR degrader 14 is a potent and selective EGFR PROTACdegrader with a DC50 of about 2.9 nM and a Dmax of 93.1% for EGFR L858R/T790M/C797S. PROTAC EGFR degrader 14 selectively induces EGFRC797S degradation through a VHL and proteasome-dependent manner and downregulated EGFR-associated transcriptome and exhibits good selectivity over EGFRWT. PROTAC EGFR degrader 14 induces cell cycle arrest and apoptosis and significantly inhibits tumor growth. PROTAC EGFR degrader 14 can be used for the study of nonsmall cell lung cancer (NSCLC) (Pink: Target protein ligand: (HY-143337) ; Blue: E3 ligand (HY-125845) ; Black: Linker (HY-W004688) ) [1].

Product Specifications

UNSPSC

12352005

Target

Apoptosis; EGFR; PROTACs

Related Pathways

Apoptosis; JAK/STAT Signaling; PROTAC; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Purity

99.26

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(CCCCCCN1CCN(C2=CC=C(NC3=NC=C4C(N(C(CNC5=CC=CC=C5)=C4)C6CCCC6)=N3)C=C2)CC1)N[C@@H](C(C)(C)C)C(N7[C@H](C(NCC8=CC=C(C9=C(C)N=CS9)C=C8)=O)C[C@@H](O)C7)=O

Molecular Formula

C57H73N11O4S

Molecular Weight

1008.33

References & Citations

[1]Wang X, et al. Discovery of a Novel EGFR PROTAC Degrader against C797S Resistance Mutation with Potent Antitumor Efficacy in NSCLC Treatment. J Med Chem. 2025 Jul 24;68 (14) :14569-14593.