Gefitinib-based PROTAC 3 - CAS 2230821-27-7

Gefitinib-based PROTAC 3 is a 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).

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Molecular Formula
Molecular Weight

Gefitinib-based PROTAC 3

    • Specification
      • Purity
        Soluble in DMSO
        White Solid
        Store at 2-8°C for short term (days to weeks) or -20°C for long term (months to years)
        Room temperature in continental US; may vary elsewhere
        IUPAC Name
        N-[3-(2-{[5-({4-[(3-Chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl}oxy)pentyl]oxy}ethoxy)propanoyl]-3-methyl-L-valyl-(4R)-4-hydroxy-N-[4-(4-methyl-1,3-thiazol-5-yl)benzyl]-L-prolinamide; L-Prolinamide, N-[3-[2-[[5-[[4-[(3-chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]oxy]pentyl]oxy]ethoxy]-1-oxopropyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)-; Iressa-based PROTAC 3; Gefitinib-based Proteolysis-targeting Chimera 3
    • Properties
      • Boiling Point
        1065.6±65.0°C at 760 Torr
        1.300±0.06 g/cm3
        InChI Key
        Canonical SMILES
    • Reference Reading
      • 1. The advantages of targeted protein degradation over inhibition: an RTK case study.
        Burslem, G.M., Smith, B.E., Lai, A.C., Jaime-Figueroa, S., McQuaid, D.C., Bondeson, D.P., Toure, M., Dong, H., Qian, Y., Wang, J. and Crew, A.P., 2018. Cell chemical biology, 25(1), pp.67-77.
        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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