Gefitinib-based PROTAC 3

SKU: orb1225618

Description

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).

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2230821-27-7
• MW: 934.522
• Purity: >98% (HPLC)
• Formula: C₄₇H₅₇ClFN₇O₈S
• SMILES: CC1=C(SC=N1)C2=CC=C(C=C2)CNC(=O)C3CC(CN3C(=O)C(C(C)(C)C)NC(=O)CCOCCOCCCCCOC4=C(C=C5C(=C4)C(=NC=N5)NC6=CC(=C(C=C6)F)Cl)OC)O
• Target: PROTAC
• Solubility: DMSO : ≥ 60 mg/mL64.20 mM

Bioactivity

• In Vitro:
  Western blot analysis. Cell line: HCC827 cells expressing exon 19 del EGFR; H3255 cells expressing L858R EGFR. Concentration: 100 nM, 250 nM, 1 μM, 2.5 μM, 10 μM for HCC827 cells; 25 nM, 100 nM, 1 μM, 2.5 μM, 10 μM for H3255 cells Incubation time: 24 hours. Result: Degradation of both exon-19 deletion EGFR as well as the mutant isoform containing the L858R activating point mutation.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

PROTAC