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Compound 56

In stock
Catalog No.
A8197
REGFR inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$190.00
In stock
Evaluation Sample
$28.00
In stock
500ug
$50.00
In stock
5mg
$150.00
In stock

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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

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt388.3
Cas No.171745-13-4
FormulaC18H18BrN3O2
Solubility≥16.95mg/mL in DMSO, ≥47.6 mg/mL in EtOH with ultrasonic, <2.45 mg/mL in H2O
Chemical NameN-(3-bromophenyl)-6,7-diethoxyquinazolin-4-amine
SDFDownload SDF
Canonical SMILESCCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=CC=C3)Br)OCC
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

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

Quality Control

Chemical structure

Compound 56

Related Biological Data

Compound 56