SJF 1521 - CAS 2230821-40-4

It is an EGFR-targeting PROTAC small molecule that can induce EGFR degradation. Epidermal growth factor receptor (EGFR), also known as ErbB1/HER1, is a proto-oncogene associated with a variety of cancers, including glioblastoma multiforme, head and neck cancer, and non-small cell lung cancer.

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Molecular Formula
C57H61ClFN7O9S
Molecular Weight
1074.65

SJF 1521

    • Specification
      • Purity
        ≥95%
        Solubility
        Soluble in DMSO
        Appearance
        Pale Green/Yellow Solid
        Storage
        Store at 2-8°C for short term (days to weeks) or -20°C for long term (months to years)
        IUPAC Name
        (2S,4R)-1-[(2S)-2-[[2-[2-[2-[2-[4-[4-[3-chloro-4-[(3-fluorophenyl)methoxy]anilino]quinazolin-6-yl]phenoxy]ethoxy]ethoxy]ethoxy]acetyl]amino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide
        Synonyms
        N-({2-[2-(2-{4-[4-({3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}amino)-6-quinazolinyl]phenoxy}ethoxy)ethoxy]ethoxy}acetyl)-3-methyl-L-valyl-(4R)-4-hydroxy-N-[4-(4-methyl-1,3-thiazol-5-yl)benzyl]-L-prolinamide; (2S,4R)-1-((S)-2-(tert-Butyl)-14-(4-(4-((3-chloro-4-((3-fluorobenzyl)oxy)phenyl)amino)quinazolin-6-yl)phenoxy)-4-oxo-6,9,12-trioxa-3-azatetradecanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide; L-Prolinamide, N-[2-[2-[2-[2-[4-[4-[[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-6-quinazolinyl]phenoxy]ethoxy]ethoxy]ethoxy]acetyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)-; EGFR PROTAC
    • Properties
      • Boiling Point
        1160.1±65.0°C at 760 Torr
        Density
        1.314±0.06 g/cm3
        InChI Key
        XZNORRXEBCTXPB-KHBXAZQSSA-N
        InChI
        InChI=1S/C57H61ClFN7O9S/c1-36-52(76-35-63-36)40-10-8-37(9-11-40)30-60-55(69)49-29-44(67)31-66(49)56(70)53(57(2,3)4)65-51(68)33-73-23-22-71-20-21-72-24-25-74-45-16-12-39(13-17-45)41-14-18-48-46(27-41)54(62-34-61-48)64-43-15-19-50(47(58)28-43)75-32-38-6-5-7-42(59)26-38/h5-19,26-28,34-35,44,49,53,67H,20-25,29-33H2,1-4H3,(H,60,69)(H,65,68)(H,61,62,64)/t44-,49+,53-/m1/s1
        Canonical SMILES
        CC1=C(SC=N1)C2=CC=C(C=C2)CNC(=O)C3CC(CN3C(=O)C(C(C)(C)C)NC(=O)COCCOCCOCCOC4=CC=C(C=C4)C5=CC6=C(C=C5)N=CN=C6NC7=CC(=C(C=C7)OCC8=CC(=CC=C8)F)Cl)O
    • 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.
Bio Calculators
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L

* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2

* Total Molecular Weight:
g/mol
Tip: Chemical formula is case sensitive. C22H30N4O c22h30n40
g/mol
g
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