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 > JBJ-02-112-05
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:
 
JBJ-02-112-05
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。
JBJ-02-112-05图片
CAS NO:2748162-29-8
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
JBJ-02-112-05 是一种有效的,突变选择性,变构和口服活性EGFR抑制剂,对EGFRL858R/T790MIC50为 15 nM。
生物活性

JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally activeEGFRinhibitor with anIC50of 15 nM forEGFRL858R/T790M[1].

IC50& Target[1]

EGFRL858R/T790M

15 nM (IC50)

体外研究
(In Vitro)

In Ba/F3 cells, JBJ-02-112-05 inhibits the activities of wildtype EGFR, EGFRL858R, EGFRL858R/T790Mand EGFRL858R/T790M/C797Swith IC50values of 9.29 μM; 8.35 μM; 8.53 μM and 2.13 μM, respectively[1].
JBJ-02-112-05 demonstrates mutant selectivity by inhibiting mutant EGFR and downstream AKT and ERK1/2 phosphorylation in Ba/F3 cells stably transfected with EGFRL858R, EGFRL858R/T790M, EGFRL858R/T790M/C797Smutations[1].

体内研究
(In Vivo)

JBJ-02-112-05 (100 mg/kg; oral gavage; once daily; for 3 days; EGFRL858R/T790M/C797Sgenetically engineered mice) treatment inhibits phosphorylation of EGFR and downstream signaling pathways[1].
JBJ-02-112-05 exhibits a moderate half-life of 3 hours and aCmaxof 13.7 μM following 3 mg/kg intravenous (i.v.) dose. A 5 mg/kg oral dose of JBJ-02-112-05 achieves a half-life of 16.4 hours and a CCmaxof 1.31 μM[1].

Animal Model:EGFRL858R/T790M/C797Sgenetically engineered mice[1]
Dosage:100 mg/kg
Administration:Oral gavage; once daily; for 3 days
Result:Inhibited phosphorylation of EGFR and downstream signaling pathways.
分子量

464.54

Formula

C27H20N4O2S

CAS 号

2748162-29-8

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.