EGFR Inhibitor

Catalog No.S0360 Synonyms: EGFR-IN-12

For research use only.

EGFR inhibitor, a cell permeable, 4,6-disubstituted pyrimidine compound, is a highly selevtive inhibitor of EGFR kinase with IC50 of 21 nM. EGFR inhibitor directly depolymerizes microtubules and is used as a chemical probe to investigate both the EGFR pathway and microtubule dynamics.

EGFR Inhibitor Chemical Structure

CAS No. 879127-07-8

Purity & Quality Control

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Biological Activity

Description EGFR inhibitor, a cell permeable, 4,6-disubstituted pyrimidine compound, is a highly selevtive inhibitor of EGFR kinase with IC50 of 21 nM. EGFR inhibitor directly depolymerizes microtubules and is used as a chemical probe to investigate both the EGFR pathway and microtubule dynamics.
Targets
Microtubules [1]
()
EGFR [1]
(Cell-free assay)
21 nM

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 83 mg/mL
(200.77 mM)
Ethanol 2 mg/mL
(4.83 mM)
Water ˂1 mg/mL

Chemical Information

Molecular Weight 413.40
Formula

C21H18F3N5O

CAS No. 879127-07-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC1C(=O)NC2=CC=CC(=C2)NC3=NC=NC(=C3)NC4=CC=CC(=C4)C(F)(F)F

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 g 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 %

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03051880 Unknown status Drug: Repair Control EGF®|Drug: Cream without rhEGF Drug-Related Side Effects and Adverse Reactions|Epidermal Growth Factor The Catholic University of Korea November 2016 Not Applicable
NCT03047863 Unknown status Drug: Repair Control EGF®|Drug: Cream without rhEGF Drug-Related Side Effects and Adverse Reactions|Epidermal Growth Factor The Catholic University of Korea November 2016 Not Applicable
NCT02588261 Terminated Drug: naquotinib mesilate|Drug: Erlotinib|Drug: Gefitinib Non-small Cell Lung Cancer (NSCLC) Astellas Pharma Global Development Inc.|Astellas Pharma Inc February 11 2016 Phase 3
NCT01892527 Unknown status Drug: Tivantinib (ARQ197) Colorectal Cancer Metastatic|C-met Overexpression Armando Santoro MD|Istituto Clinico Humanitas March 2013 Phase 2

(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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