化学信息：
| 化学名 | N-(3-bromophenyl)-6,7-dimethoxyquinazolin-4-amine;hydrochloride |
|
| 简称 | PD153035 | |
| 别名 |
ZM 252868, AG 1517, Tyrphostin AG 1517, SU 5271, PD-153035, PD 153035 |
|
| 中文名 | N/A | |
| 化学式 | C16H15BrClN3O2 | |
| 分子量 | 396.67 | |
| CAS号 | 183322-45-4 | |
| 纯度 | 98% | |
| 溶剂/溶解度 |
Water<1.2mg/ml; DMSO 4mg/ml warming; Ethanol<1.2mg/ml |
|
| 溶液配制 | 5mg加入1.26ml DMSO，或者每3.97mg加入1ml DMSO，配制成10mM溶液。SD4744-10mM用DMSO配制。 |
生物信息：
| 产品描述 | PD153035 HCl (ZM 252868; AG 1517) is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2pM and 29pM; little effect against PGDFR, FGFR, CSF-1, InsR and Src. | ||||
| 信号通路 | JAK/STAT | ||||
| 靶点 | EGFR | － | － | － | － |
| IC50 | 5.2/29 pM(Ki/IC50) | － | － | － | － |
| 体外研究 | PD 153035 shows a potent and selective inhibitory effect on tyrosine phosphorylation induced with EGF with IC50 of 15nM and 14nM in Swiss 3T3 fibroblast and A-431 human epidermoid carcinoma cells, respectively. PD153035 shows growth inhibitory effects in cultures of EGF receptor-overexpressing human cancer cell lines including A431, Difi, DU145, MDA-MB-468 and ME180 cells with IC50 of 0.22μM, 0.3μM, 0.4μM, 0.68μM and 0.95μM, respectively. | ||||
| 体内研究 | In A431 human epidermoid tumors grown as xenografts in immunodeficient nude mice, PD153035 at 80mg/kg inhibit EGF receptor tyrosine kinase activity. PD153035 improves glucose tolerance, insulin sensitivity，and signaling and reduces subclinical inflammation in HFD-fed mice. | ||||
| 临床实验 | N/A | ||||
| 特征 | N/A | ||||
相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
| 酶活性检测实验 | |
| 方法 | N/A |
| 细胞实验 | |
| 细胞系 | N/A |
| 浓度 | N/A |
| 处理时间 | N/A |
| 方法 | N/A |
| 动物实验 | |
| 动物模型 | N/A |
| 配制 | N/A |
| 剂量 | N/A |
| 给药方式 | N/A |
| 产品编号 | 产品名称 | 包装 |
| SD4744-10mM | PD153035 (EGFR抑制剂) | 10mM×0.2ml |
| SD4744-5mg | PD153035 (EGFR抑制剂) | 5mg |
| SD4744-25mg | PD153035 (EGFR抑制剂) | 25mg |
| — | 说明书 | 1份 |
保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
