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 > Rezivertinib
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:
 
Rezivertinib
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。
Rezivertinib图片
CAS NO:1835667-12-3
包装与价格:
包装价格(元)
25 mg电议
50 mg电议
100 mg电议

产品介绍

产品描述

Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity[1][2].

体外活性

Rezivertinib (BPI-7711) selectively inhibits cellular proliferation of EGFR mutations in cell lines: GI50 13.3 nM (PC9, del19), 6.8 nM (HCC827, L858R), 22 nM (NCI-H1975, del19/T790M) and >1000 nM (A431, EGFR WT)[1].

体内活性

Rezivertinib (BPI-7711; 6.25-25 mg/kg/day; orally; 14 days) shows significant tumor regression[2]. Rezivertinib (12.5 mg/kg/day; orally; 14 days) survives an average of 112% longer in H1975-luc human NSCLC mice model[2]. Rezivertinib (50 mg/kg/day; orally) has anti-tumor efficacy correlated to improved average overall survival of the animals of 115% (28 days vs. 13 days)[2].

Cas No.

1835667-12-3

分子式

C27H30N6O3

分子量

486.57

别名

Rezivertinib

储存和溶解度

DMSO:125 mg/mL (256.90 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years