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Gefitinib-based PROTAC 3

Chemical Structure : Gefitinib-based PROTAC 3

CAS No.: 2230821-27-7

Gefitinib-based PROTAC 3

Catalog No.: PC-35357Not For Human Use, Lab Use Only.

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)..

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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).

Physicochemical Properties

M.Wt 934.522
Formula C47H57ClFN7O8S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2S,4R)-1-((S)-2-(3-(2-((5-((4-((3-chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)pentyl)oxy)ethoxy)propanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide

References

1. Burslem GM, et al. Cell Chem Biol. 2018 Jan 18;25(1):67-77.e3.

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