您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Nazartinib mesylate
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Nazartinib mesylate
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。
Nazartinib mesylate图片
CAS NO:1508250-72-3
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
EGF816 mesylate
产品介绍
Nazartinib mesylate (EGF816 mesylate) 是一种新颖的EGFR抑制剂,对 EGFR(L858R/790M) 突变体的KiKinact值分别为 31 nM 和 0.222 min–1
生物活性

Nazartinib mesylate (EGF816 mesylate) is a novel, covalent mutant-selectiveEGFRinhibitor, withKiandKinactof 31 nM and 0.222 min–1on EGFR(L858R/790M) mutant, respectively.

IC50& Target[1]

EGFRL858R/T790M

31 nM (Ki)

体外研究
(In Vitro)

Nazartinib (EGF816) has inhibitory effect on the mutant cell lines with IC50s of 4, 6, 2 nM in H1975, H3255, and HCC827, respectively, and demonstrates improved ADME and PK properties[1]. Nazartinib (EGF816) shows potent inhibition of pEGFR levels in H3255, HCC827, and H1975 cell lines with EC50values of 5, 1, and 3 nM, respectively. Nazartinib inhibits cell proliferation, with EC50values of 9, 11, and 25 nM in H3255, HCC827, and H1975, respectively. Nazartinib has an OC50(compound concentration at 50% occupancy) value of 2 and 5 nM on HCC827 and H1975, respectively[2].

体内研究
(In Vivo)

In H1975 mouse xenograft model, Nazartinib (EGF816; 50 and 20 mg/kg or 25 mg/kg, p.o.) demonstrates dose-dependent efficacy with near complete tumor cells regression at the highest dose tested (50 mg/kg)[1]. In H1975 mouse model, Nazartinib (EGF816; 10 mg/kg, p.o.) induces tumor growth inhibition with a T/C (tumor/control volume) of 29%, and when doses are 30 and 100 mg/kg, tumor regressions are achieved (T/C, –61% and –80%, respectively). In the H3255 xenograft model, Nazartinib (30 mg/kg, p.o.) shows significant antitumor activity. Antiproliferative activity of Nazartinib on 89 lung cancer cell lines indicates that Nazartinib selectively inhibits cell lines containing EGFR with catalytic domain mutations[2].

Clinical Trial
分子量

591.12

Formula

C27H35ClN6O5S

CAS 号

1508250-72-3

中文名称

那扎替尼甲磺酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.