化学信息：
| 化学名 | N-(3-ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin-4-amine hydrochloride |
|
| 简称 | Icotinib HCl | |
| 别名 |
Icotinib Hydrochloride, BPI-2009H |
|
| 中文名 | 凯美纳 | |
| 化学式 | C22H22ClN3O4 | |
| 分子量 | 427.88 | |
| CAS号 | 1204313-51-8 | |
| 纯度 | 98% | |
| 溶剂/溶解度 |
Water<1mg/ml; DMSO5mg/ml; Ethanol<1mg/ml |
|
| 溶液配制 | 5mg加入1.17ml DMSO，或者每4.28mg加入1ml DMSO，配制成10mM溶液。SD4767-10mM用DMSO配制。 |
生物信息：
| 产品描述 | Icotinib hydrochloride is a potent and specific epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with an IC(50) of 5nM, including it's mutants of EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R). | ||||
| 信号通路 | JAK/STAT; Protein Tyrosine Kinase | ||||
| 靶点 | EGFR and EGFR mutants | － | － | － | － |
| IC50 | 5nM | － | － | － | － |
| 体外研究 | Icotinib inhibits EGFR activity in a dose-dependent manner, with an IC50value of 5nM and complete inhibition at 62.5nM. Icotinib selectively solely inhibits the EGFR members including the wild type and mutants with inhibition efficacies of 61-99%. Icotinib blocks EGFR-mediated intracellular tyrosine phosphorylation in human epidermoid carcinoma A431 cells in a dose-dependent manner. Meanwhile, in our proliferation assay performed on A431, BGC-823, A549, H460, HCT8, KB and Bel-7402 cell lines, we found that the relative sensitivity of cell lines to Icotinib is A431 > BGC-823 > A549 > H460 > KB > HCT8 and Bel-7402. Icotinib exhibits a broad spectrum of antitumor activity and it is especially effective against tumors expressing higher levels of EGFR. | ||||
| 体内研究 | In vivo studies demonstrated that Icotinib exhibited potent dose-dependent antitumor effects in nude mice carrying a variety of human tumor-derived xenografts. The drug was well tolerated at doses up to 120mg/kg/day in mice without mortality or significant body weight loss during the treatment. A head to head randomized, double blind phase III trial using Gefitinib as an active control for patients with advanced non-small cell lung cancer (NSCLC) was finished recently (Trial registration ID: NCT01040780). | ||||
| 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 |
| SD4767-10mM | Icotinib HCl (EGFR抑制剂) | 10mM×0.2ml |
| SD4767-5mg | Icotinib HCl (EGFR抑制剂) | 5mg |
| SD4767-25mg | Icotinib HCl (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。
