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Supplier NameMedChemExpress (MCE)
Contactsales
Tel609-228-6898
Mobile609-228-6898
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Emailsales@medchemexpress.com; tech@medchemexpress.com
Websitehttps://www.medchemexpress.com/
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Product NameGefitinib-based PROTAC 3
SynonymsNTN21277;Gefitinib-based PROTAC 3;NTN21277(Gefitinib-based PROTAC 3)
CAS2230821-27-7
EINECS
Chemical FormulaC47H57ClFN7O8S
Molecular Weight934.52
inchi
Package1 mg;5 mg;10 mg;25 mg;50 mg
PriceGet quote
DescriptionsGefitinib-based PROTAC 3

Gefitinib-based PROTAC 3

MedChemExpress (MCE)

HY-123921

2230821-27-7

99.98%

4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months

Descriptions

Gefitinib-based PROTAC 3

Gefitinib-based PROTAC 3

MedChemExpress (MCE)

HY-123921

2230821-27-7

99.98%

4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months
-20°C, 1 month (sealed storage, away from moisture and light)

Room temperature in continental US
may vary elsewhere.

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.

H3255 cells expressing L858R EGFR treated with Gefitinib-based PROTAC 3 (25 nM-10 μM
24 hours), HCC827 cells expressing exon 19 del EGFR treated with Gefitinib-based PROTAC 3 (100 nM-10 μM
24 hours), which enables the degradation of both exon-19 deletion EGFR as well as the mutant isoform containing the L858R activating point mutation, while sparing the WT EGFR[1].

EGFR 11.7 nM (DC50, HCC827(exon 19 del) cells) EGFR 22.3 nM (DC50, H3255 (L858R mutantion) cells) PROTAC

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[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.
[Content Brief]

Supplier Websitehttps://www.medchemexpress.com/gefitinib-based-protac-3.html
Last Update2025-05-21 16:50:25
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