Gefitinib-based PROTAC 3

Catalog No.S0070

For research use only.

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 No. 2230821-27-7

Purity & Quality Control

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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)

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(107.0 mM)
Ethanol 100 mg/mL
(107.0 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 934.51
Formula
C47H57ClFN7O8S
CAS No. 2230821-27-7
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01164735 Not yet recruiting Other: Laboratory Biomarker Analysis 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 --
NCT05139290 Not yet recruiting Behavioral: Prototype Intervention Dementia|Alzheimer Disease|Caregiver Burden Emory University|National Institute on Aging (NIA) December 2024 Not Applicable
NCT04576663 Not yet recruiting Drug: Normal saline|Drug: Phenylephrine Adverse Effect General Hospital of Ningxia Medical University October 1 2023 Not Applicable
NCT05105386 Not yet recruiting Device: SynAir-Child Pollution; Exposure|Environmental Exposure|Childhood Asthma|Childhood National and Kapodistrian University of Athens September 2023 --
NCT04571502 Not yet recruiting Other: CareHeroes Neurocognitive Disorders|Alzheimer Disease|Caregiver Florida International University|National Institute on Aging (NIA)|University of Alabama Tuscaloosa September 2023 Not Applicable

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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