Gefitinib-based PROTAC 3

• CAS Number:

  2230821-27-7

• UNSPSC Description:

  Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a von Hippel-Lindau ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively[1].

• Target Antigen:

  EGFR; PROTACs

• Type:

  Reference compound

• Related Pathways:

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

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/gefitinib-based-protac-3.html

• Purity:

  99.98

• Solubility:

  DMSO : ≥ 60 mg/mL

• 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

• Molecular Weight:

  934.51

• References & Citations:

  [1]Burslem GM, et al. The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study. Cell Chem Biol. 2018 Jan 18;25(1):67-77.e3.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  4°C (Powder, sealed storage, away from moisture and light)

• Clinical Information:

  No Development Reported