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
|
参考文献：
1. Tan F, et al. Lung Cancer. 2012 May, 76(2), 177-82.
包装清单：
|
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。
注意事项：
本产品对人体有害，操作时请小心，并注意有效防护以避免直接接触人体或吸入体内。
本产品仅限于专业人员的科学研究用，不得用于临床诊断或治疗，不得用于食品或药品，不得存放于普通住宅内。
为了您的安全和健康，请穿实验服并戴一次性手套操作。
微信在线咨询
微信在线咨询
