Gefitinib-based PROTAC 3
This bifunctional PROTAC molecule, designated as compound 3, utilizes a gefitinib-derived warhead to target EGFR and a VHL ligand to recruit the cellular degradation machinery. It potently induces degradation of mutant EGFR proteins in NSCLC cell lines, including HCC827 (exon 19 del) and H3255 (L858R), with DC50 values in the low nanomolar range. This tool compound is valuable for probing targeted protein degradation in oncology research, both in vitro and in vivo.
Product Specifications
CAS Number
2230821-27-7
Product Name Alternative
Inhibitor, Gefitinib based PROTAC 3, Gefitinibbased PROTAC 3, Gefitinib-based PROTAC 3, HER1, ErbB-1, EGFR, Epidermal growth factor receptor, inhibit, PROTACs
Field of Research
Cardiovascular Research, Pharmacology & Drug Discovery, Signal Transduction
Purity
97.29% (May vary between batches)
Solubility
DMSO:10 mM
Smiles
N (C=1C2=C (C=C (OC) C (OCCCCCOCCOCCC (N[C@H] (C (=O) N3[C@H] (C (NCC4=CC=C (C=C4) C=5SC=NC5C) =O) C[C@@H] (O) C3) [C@] (C) (C) C) =O) =C2) N=CN1) C6=CC (Cl) =C (F) C=C6
Molecular Formula
C47H57ClFN7O8S
Molecular Weight
934.51
Storage Conditions
-20°C
Notes
For research use only.
Available Sizes
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