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PD153035 (SU-5271; AG1517; ZM 252868) 是有效地 EGFR 抑制剂,Ki 和 IC50 值分别为6和25 pM。
中文别名:
4-[(3-溴苯基)氨基]-6,7-二甲氧基喹啉;
4-[(3-溴苯基)氨基]-6,7-二甲氧基喹唑啉盐酸盐;
N-(3-溴苯基)-6,7-二甲氧基喹唑啉-4-胺
物化属性:
密度:1.499
沸点:472.1°C at 760 mmHg
折射率:1.679
闪光点:239.3°C
[1]. Bridges AJ, et al. 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. 1996 Jan 5;39(1):267-76.
[2]. Fry DW, et al. A specific inhibitor of the epidermal growth factor receptor tyrosine kinase. Science. 1994 Aug 19;265(5175):1093-5.
[3]. Bos M, et al. PD153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptoractivation and inhibits growth of cancer cells in a receptor number-dependent manner. Clin Cancer Res. 1997 Nov;3(11):2099-106.
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