• We specialize in small molecule inhibitors, agonists, antagonists and screening libraries!
Search Site
Related Products
Compound 56REGFR inhibitor

Compound 56

Catalog No. A8197
Size Price Stock Qty
10mM (in 1mL DMSO) $190.00 In stock
Evaluation Sample $28.00 In stock
500µg $50.00 In stock
5mg $150.00 In stock

Tel: +1-832-696-8203

Email: sales@apexbt.com

Worldwide Distributors

Sample solution is provided at 25 µL, 10mM.

Quality Control

Chemical structure

Compound 56

Biological Activity

Description Compound 56 is a cell-permeable, reversible, and ATP-competitive inhibitor of tyrosine kinase activity of EGFR.
Targets EGFR          
IC50            

Compound 56 Dilution Calculator

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

calculate

Compound 56 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Chemical Properties

Cas No. 171745-13-4 SDF Download SDF
Chemical Name N-(3-bromophenyl)-6,7-diethoxyquinazolin-4-amine
Canonical SMILES CCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=CC=C3)Br)OCC
Formula C18H18BrN3O2 M.Wt 388.3
Solubility >16.95mg/mL in DMSO Storage Store at -20°C
General tips N/A
Shipping Condition N/A

Background

Compound 56, 4-[(3-Bromophenyl)amino]-6,7-diethoxyquinazoline, is a potent and specific inhibitor of the tyrosine kinase of the epidermal growth factor receptor (EGFR) showing an IC50 of 0.006 nM. It competitively binds at the adenosine-triphosphate (ATP) site of EGFR. Compound 56 is capable of inhibiting the phosphorylation of EGF-dependent EGFR, suppressing the proliferation and clonogenicity of a wide panel of EGFR-overexpressing human cancer lines, and blocking EGF-mediated mitogenesis and oncogenic transformation in fibroblasts overexpressing EGFR. Besides inhibiting EGFR tyrosine kinase, It also inhibits the tyrosine kinase of human epidermal growth factor receptor 2 (HER2/neu) but with a less potency.

Reference

Bridges AJ, Zhou H, Cody DR, Rewcastle GW, McMichael A, Showalter HD, Fry DW, Kraker AJ, and Denny WA. Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor.J Med Chem 1966; 39 (1): 267-276

Monique Bos, Jhn Mendelsohn, Young-Mee Kim, Joan Albanell, David W. Fry, and Jose Baelga. PD153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptor activation and inhibits growth of cancer cells in a receptor number-dependent manner. Clin Cancer Res 1997;3:2099-2106