Name: Gefitinib-based PROTAC 3
Brand: Selleck Chemicals
SKU: S0070
Rating: 5 (1 reviews)

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

CAS: 2230821-27-7

Purity & Quality Control

Batch: Purity: 99.99%

99.99

Gefitinib-based PROTAC 3 Related Products

Related Targets	EGFR/ErbB1 HER2/ErbB2 ErbB3 ErbB4 mutant EGFR	Click to Expand
Related Compound Libraries	Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library PI3K/Akt Inhibitor Library Cell Cycle compound library Angiogenesis Related compound Library	Click to Expand

Signaling Pathway

EGFR Signaling Pathway

Choose Selective EGFR Inhibitors

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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References

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

Chemical Information & 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	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

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
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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% DMSO + % + % Tween 80 + % ddH₂O

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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. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

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

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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