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产品介绍
产品介绍
产品信息
抗原名称
EGFRWT:190 nM, EGFRdel19 T790M C797S:0.2 nM, EGFRdel19:1 nM

商品描述
BI-4020 is a fourth-generation, orally active, and non-covalent inhibitor of EGFR tyrosine kinase. BI-4020 exhibits activity agains the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines), the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM) and EGFR wt (IC50=190 nM). BI-4020 exhibits high kinome selectivity and good DMPK properties.

分子量
542.68

纯度
98%

可溶性
DMSO:240 mg/mL (442.25 mM)

In vitro(体外研究)
BI-4020 inhibits p-EGFR del19 T790M C797S ( IC50: 0.6 nM). BI-4020 inhibits not only the triple mutant EGFR (del19/T790M/C797S) variant (IC50=0.2 nM in BaF3 cell lines) but also the double mutant EGFR (del19/T790M) and primary mutant EGFR del19 (IC50: 1 nM). BI-4020 also shows activity against EGFR wt (IC50: 190 nM). BI-4020 shows high kinome selectivity and good DMPK properties.

In vivo(体内研究)
In the human PC-9 (EGFR del19/T790M/C797S) triple mutant NSCLC xenograft model in mice, BI-4020 leads to tumor regressions.

背景
分子式
C30H38N8O2

CAS号
2664214-60-0

制备和贮存
保存方式
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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