BI-4020 是第四代非共价口服活性 EGFR 酪氨酸激酶抑制剂。

BI-4020 is a fourth-generation, non-covalent, and orally active inhibitor of EGFR tyrosine kinase.

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

2664214-60-0

C30H38N8O2

542.68

DMSO:240 mg/mL (442.25 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years