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Compound 56
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Compound 56图片
CAS NO:171745-13-4
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
500μg电议
5mg电议

产品介绍

REGFR inhibitor

Cas No.171745-13-4
别名N-(3-溴苯基)-6,7-二乙氧基-4-喹唑啉胺
化学名N-(3-bromophenyl)-6,7-diethoxyquinazolin-4-amine
Canonical SMILESCCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=CC=C3)Br)OCC
分子式C18H18BrN3O2
分子量388.3
溶解度≥ 16.95mg/mL in DMSO, ≥ 47.6 mg/mL in EtOH with ultrasonic
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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 IC50of 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