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Compound 56

Katalog-Nr.GC12837

A potent EGFR inhibitor

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Compound 56 Chemische Struktur

Cas No.: 171745-13-4

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10mM (in 1mL DMSO)
139,00 $
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500μg
35,00 $
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5mg
107,00 $
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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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

[1].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
[2].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

Chemical Properties

Cas No. 171745-13-4 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
Löslichkeit ≥ 16.95mg/mL in DMSO, ≥ 47.6 mg/mL in EtOH with ultrasonic Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.5753 mL 12.8766 mL 25.7533 mL
5 mM 0.5151 mL 2.5753 mL 5.1507 mL
10 mM 0.2575 mL 1.2877 mL 2.5753 mL
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Review for Compound 56

Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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