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Gefitinib hydrochloride EGFR inhibitor

Cat.No.S5098

Gefitinib (ZD1839) is an EGFR inhibitor with IC50s of 15.5 nM and 823.3 nM for WT EGFR and EGFR (858R/T790M), respectively.
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Quality Control

Batch: Purity: 99.94%
99.94

Solubility

In vitro
Batch:

DMSO : 4 mg/mL (8.27 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 1 mg/mL

Ethanol : 1 mg/mL

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Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg
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μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO
%
% Tween 80
% ddH2O
% DMSO
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Calculation results:

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.

Chemical Information, Storage & Stability

Molecular Weight 483.36 Formula

C22H24ClFN4O3.HCl

Storage (From the date of receipt)
CAS No. 184475-55-6 -- Storage of Stock Solutions

Synonyms ZD1839 hydrochloride SMILES COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4.Cl

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
EGFR
(Cell-free assay)
15.5 nM
EGFR (858R/T790M)
(Cell-free assay)
823.3 nM
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-03-09)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07458919 NOT_YET_RECRUITING
Lung Cancer
Fuzhou General Hospital
2026-03-30 EARLY_PHASE1
NCT07477457 RECRUITING
Osteosarcoma; Metastasis
Memorial Sloan Kettering Cancer Center
2026-03-11 PHASE2
NCT03040973 ACTIVE_NOT_RECRUITING
Advanced Solid Tumors Which Are cMET-dependent
Novartis Pharmaceuticals
2017-08-23 PHASE2
NCT03333343 ACTIVE_NOT_RECRUITING
EGFR-mutant Non-small Cell Lung Cancer
Novartis Pharmaceuticals
2018-01-29 PHASE1
NCT03122717 ACTIVE_NOT_RECRUITING
Non-Small Cell Lung Cancer
Dana-Farber Cancer Institute
2017-05-09 PHASE1; PHASE2
NCT06071013 RECRUITING
Non-small Cell Lung Cancer; EGFR Gene Mutation; EGFR-TKI Resistant Mutation
China Medical University Hospital
2024-02-23 PHASE1; PHASE2

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