EGFR Inhibitor

Synonyms: EGFR-IN-12

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

EGFR Inhibitor Chemical Structure

CAS: 879127-07-8

Selleck's EGFR Inhibitor has been cited by 2 publications

Purity & Quality Control

Batch: S036001 DMSO] 83 mg/mL] false] Ethanol] 2 mg/mL] false] Water] ˂1 mg/mL] false Purity: 99.56%
99.56

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Signaling Pathway

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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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06118047 Recruiting
Metastatic Colorectal Cancer|Cetuximab|Skin Toxicity
Sun Yat-sen University
August 1 2023 Phase 2
NCT03051880 Unknown status
Drug-Related Side Effects and Adverse Reactions|Epidermal Growth Factor
The Catholic University of Korea
November 2016 Not Applicable
NCT03047863 Unknown status
Drug-Related Side Effects and Adverse Reactions|Epidermal Growth Factor
The Catholic University of Korea
November 2016 Not Applicable
NCT02588261 Terminated
Non-small Cell Lung Cancer (NSCLC)
Astellas Pharma Global Development Inc.|Astellas Pharma Inc
February 11 2016 Phase 3

Chemical Information & Solubility

Molecular Weight 413.40 Formula

C21H18F3N5O

CAS No. 879127-07-8 SDF --
Smiles C1CC1C(=O)NC2=CC=CC(=C2)NC3=NC=NC(=C3)NC4=CC=CC(=C4)C(F)(F)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 83 mg/mL ( (200.77 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : ˂1 mg/mL


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

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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