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SJF1528 | Degrader (PROTAC) of EGFR, ERBB2
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
EGFR
    • DC 50:39.2 nM
    • Dmax:97.6 %
    ERBB2
      • DC 50:736.2 nM
      • Dmax:68.8 %
      Degrader (PROTAC)
      250 nM

      Selectivity

      In Cell Selectivity Assessment
      Selectivity Assessment Description:
      Potent degrader of both EGFR and HER2

      Potency
      Cellular
      In Vitro

      EGFR

      Mode of Action: Degrader (PROTAC)

      Structure-Activity-Relationship data available? No

      DOI Reference: 10.1016/j.chembiol.2017.09.009

      ERBB2

      Mode of Action: Degrader (PROTAC)

      Structure-Activity-Relationship data available? No

      DOI Reference: 10.1016/j.chembiol.2017.09.009

      Orthogonal Probes def

      Canertinib
      Afatinib
      Lapatinib

      Chemical Information

      Molecular Formula C55H57ClFN7O8S
      SMILEs Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCOCCOc2ccc(-c3ccc4ncnc(Nc5ccc(OCc6cccc(F)c6)c(Cl)c5)c4c3)cc2)C(C)(C)C)cc1
      InChI InChI=1S/C55H57ClFN7O8S/c1-34-50(73-33-61-34)38-10-8-35(9-11-38)28-58-53(67)47-27-42(65)29-64(47)54(68)51(55(2,3)4)63-49(66)31-70-21-20-69-22-23-71-43-16-12-37(13-17-43)39-14-18-46-44(25-39)52(60-32-59-46)62-41-15-19-48(45(56)26-41)72-30-36-6-5-7-40(57)24-36/h5-19,24-26,32-33,42,47,51,65H,20-23,27-31H2,1-4H3,(H,58,67)(H,63,66)(H,59,60,62)/t42-,47+,51-/m1/s1
      Molecular weight 1029.37 Da
      AlogP 0.0
      HBond acceptors 15
      HBond donors 4
      Atoms 130

      References

      Publications

      Cross References

      canSARChEMBLBindingDB

      Vendors

      Note: This is not an exhaustive list and does not indicate endorsement by the portal.

      Expert Reviews

      by SERP
      (on 9 Feb 2021 )
      Cellular Use Rating
      Reviewer notes: The biochemical potencies listed above are approximately that of lapatinib (Chembl lists the IC50 of lapatinib on EGFR and HER2 to be between 2 < IC50 < 10 nM depending on...
      by SERP
      (on 10 Feb 2021 )
      Cellular Use Rating
      This probe is highly recommended for the purposes of studying the phenotypic outcomes of degradation of HER-2 (ERBB2), EGFR, L858R or Exon 19 del EGFR in cells. Other than these RTK targets, as a result...
      by SERP+
      (on 31 Oct 2024 )
      Cellular Use Rating
      Although this compound is based on Lapatinip - one the most selective kinase inhibitors - this PROTAC may have some off-target activities; as a result, it is highly recommended that the PROTAC be evaluated...
      Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria