(Rac)-JBJ-04-125-02 是 JBJ-04-125-02 的消旋体,是选择性突变,可口服的 EGFR 变构抑制剂,对EGFRL858R/T790M的IC50为 0.26 nM。
产品描述
JBJ-04-125-02 is effective as a single agent in both in vitro and in vivo models of EGFR-mutant lung cancer.
体外活性
(Rac)-JBJ-04-125-02 is the racemate of JBJ-04-125-02. JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFRL858R/T790M[1].
体内活性
The combination of osimertinib and JBJ-04-125-02 is a significantly more effective treatment approach than either agent alone[1].
动物实验
Ba/F3, H1975, H3255GR and H3255DR cells were treated with increasing concentrations of inhibitors for 72 hours and growth or the inhibition of growth was assessed by MTS assay according to previously established methods.
Cas No.
2140807-05-0
分子式
C29H26FN5O3S
分子量
543.62
别名
JBJ-04-125-02;(Rac)-JBJ-04-125-02
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years