产品
编 号:F741712
分子式:C30H38N8O2
分子量:542.68
产品类型
结构图
CAS No: 2664214-60-0
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产品详情
生物活性:
BI-4020 is a fourth-generation, orally active, and non-covalent EGFR tyrosine kinase inhibitor. 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.
体内研究:
BI-4020 leads to tumor regressions in the human PC-9 (EGFR del19 T790M C797S) triple mutant NSCLC xenograft model in mice.
体外研究:
BI-4020 inhibits p-EGFR del19 T790M C797S with an IC50 of 0.6 nM.