Home Protein Tyrosine Kinase EGFR inhibitor - PROTAC chemical Gefitinib-based PROTAC 3 For research use only.

Gefitinib-based PROTAC 3

Gefitinib-based PROTAC 3 which conjugates an EGFR binding element to a VHL ligand via a linker induces degradation of EGFR and mutants with DC50 of 11.7 nM and 22.3 nM in HCC827(Exon 19 del) and H3255 (L858R) cells, respectively.

Gefitinib-based PROTAC 3 Chemical Structure

Gefitinib-based PROTAC 3 Chemical Structure

CAS: 2230821-27-7

Purity & Quality Control

Batch: Purity: 99.99%
99.99

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Biological Activity

Description Gefitinib-based PROTAC 3 which conjugates an EGFR binding element to a VHL ligand via a linker induces degradation of EGFR and mutants with DC50 of 11.7 nM and 22.3 nM in HCC827(Exon 19 del) and H3255 (L858R) cells, respectively.
Targets
EGFR [1]
(in HCC827(Exon 19 del) cells)		 EGFR [1]
(in H3255 (L858R) cells)
11.7 nM(DC50) 22.3 nM(DC50)
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01164735 Not yet recruiting Recurrent Uterine Corpus Carcinoma|Stage III Uterine Corpus Cancer|Stage IV Uterine Corpus Cancer Gynecologic Oncology Group|National Cancer Institute (NCI)|GOG Foundation January 2100 --
NCT05763030 Not yet recruiting Child Sleep New York State Psychiatric Institute|International Centre for Diarrhoeal Disease Research Bangladesh|Fogarty International Center of the National Institute of Health April 2027 Not Applicable
NCT06134076 Not yet recruiting Fermented Food|Inflammation Penn State University|USDA ARS September 2025 Not Applicable

Chemical lnformation & Solubility

Molecular Weight 934.51 Formula
C47H57ClFN7O8S
CAS No. 2230821-27-7 SDF --
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
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (107.0 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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