1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
    Apoptosis
  2. EGFR
    Apoptosis
  3. EGFR kinase inhibitor 1

EGFR kinase inhibitor 1 

Cat. No.: HY-143246
Handling Instructions

EGFR kinase inhibitor 1 is a potent EGFR inhibitor with IC50s of 37, 1.7, >300 nM for WT, l885R/T790M, L858R/T790M/C797S, respectively. EGFR kinase inhibitor 1 induces apoptosis and cell cycle arrest at G0/G1-phase. EGFR kinase inhibitor 1 inhibits the cell motility. EGFR kinase inhibitor 1 shows antiproliferative and anti-tumor activity.

For research use only. We do not sell to patients.

EGFR kinase inhibitor 1 Chemical Structure

EGFR kinase inhibitor 1 Chemical Structure

CAS No. : 2413958-04-8

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

EGFR kinase inhibitor 1 is a potent EGFR inhibitor with IC50s of 37, 1.7, >300 nM for WT, l885R/T790M, L858R/T790M/C797S, respectively. EGFR kinase inhibitor 1 induces apoptosis and cell cycle arrest at G0/G1-phase. EGFR kinase inhibitor 1 inhibits the cell motility. EGFR kinase inhibitor 1 shows antiproliferative and anti-tumor activity[1].

IC50 & Target[1]

EGFR (WT)

37 nM (IC50)

EGFRL858R/T790M

1.7 nM (IC50)

EGFRL858R/T790M/C797S

>300 nM (IC50)

In Vitro

EGFR kinase inhibitor 1 (compound 17i) (72 h) shows antiproliferative activity with IC50s of 4.17, 0.052 µM for A549, H1975 cells, respectively[1].
EGFR kinase inhibitor 1 (0.05, 0.5, 5 µM; 48 h) induces apoptosis in a dose-dependent manner[1].
EGFR kinase inhibitor 1 (4, 20, 100 nM; 48 h) induces cell cycle arrest at G0/G1-phase[1].
EGFR kinase inhibitor 1 (0.5 μM; 0, 24, 48 h) inhibits the motility of the H1975 cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1]

Cell Line: A549, H1975 cells
Concentration:
Incubation Time: 72 h
Result: Showed antiproliferation activity with IC50s of 4.17, 0.052 µM for A549, H1975 cells, respectively.

Apoptosis Analysis[1]

Cell Line: H1975 cells
Concentration: 0.05, 0.5, 5 µM
Incubation Time: 48 h
Result: Induced apoptosis in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: H1975 cells
Concentration: 4, 20, 100 nM
Incubation Time: 48 h
Result: Induced cell cycle arrest at G0/G1-phase with the percentage of G0/G1-phase cells increased from 42.93% to 60.52% at 4 nM, 70.39% at 20 nM and 80.03% at 100 nM.
Molecular Weight

521.61

Formula

C30H31N7O2

CAS No.
SMILES

C=CC(NC1=C(C=C(C(NC2=NC(C3=CN(C4=C3C=CC=C4)C)=CC=N2)=C1)OC)N5C=CC=C5CN(C)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
EGFR kinase inhibitor 1
Cat. No.:
HY-143246
Quantity:
MCE Japan Authorized Agent: