Gefitinib-based PROTAC 3

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