Gefitinib-based PROTAC 3

- Overview
  - Gefitinib-based PROTAC 3 is a novel, potent and selective VHL-recruiting PROTAC that induces the degradation of EGFR and EGFR mutants with DC50 of 11.7 nM and 22.3 nM for HCC827 cell (Exon 19 del) and H3255 cell (L858R). Proteolysis targeting chimera (PROTAC) technology has emerged over the last two decades as a powerful tool for targeted degradation of endogenous proteins. Herein we describe the development of PROTACs for receptor tyrosine kinases, a protein family yet to be targeted for induced protein degradation. The use of VHL-recruiting PROTACs against this protein family reveals several advantages of degradation over inhibition alone: direct comparisons of fully functional, target-degrading PROTACs with target-inhibiting variants that contain an inactivated E3 ligase-recruiting ligand show that degradation leads to more potent inhibition of cell proliferation and a more durable and sustained downstream signaling response, and thus addresses the kinome rewiring challenge seen with many receptor tyrosine kinase inhibitors. Combined, these findings demonstrate the ability to target receptor tyrosine kinases for degradation using the PROTAC technology and outline the advantages of this degradation-based approach.
    
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- Properties
  - Categories
    
    PROTACs
    
    CAS Number
    
    2230821-27-7
    
    Molecular Formula
    
    C47H57CLFN7O8S
    
    Molecular Weight
    
    934.51
    
    Purity
    
    ≥98%
    
    Storage
    
    Powder: store in -20°C freezer for up to three years, store in 4°C freezer for up to two years
    In solvent: store in -80°C freezer for up to six months, store in -20°C freezer for up to two months
    
    Shipping
    
    Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
    
    SMILES
    
    O=C([C@H]1N(C([C@@H](NC(CCOCCOCCCCCOC2=CC3=C(NC4=CC=C(F)C(Cl)=C4)N=CN=C3C=C2OC)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC5=CC=C(C6=C(C)N=CS6)C=C5
    
    * For research use only

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