Gefitinib-based PROTAC 3

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].

Product Specifications

CAS Number

[2230821-27-7]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

EGFR; PROTACs

Type

Reference compound

Related Pathways

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

Applications

Cancer-Kinase/protease

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 Formula

C47H57ClFN7O8S

Molecular Weight

934.51

Precautions

H302, H315, H319, H335

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.