BI-4020 是第四代口服活性非共价 EGFR 酪氨酸激酶抑制剂。 BI-4020 不仅抑制三突变 EGFR del19 T790M C797S 变体（在 BaF3 细胞系中 IC50=0.2 nM），而且抑制双突变 EGFR del19 T790M 和原发突变 EGFR del19 (IC50=1 nM)。 BI-4020 还显示出针对 EGFR wt (IC50=190 nM) 的活性。 BI-4020 显示出高激酶组选择性和良好的 DMPK 特性。
货号:ajcx14754
CAS:N/A
分子式:C30H38N8O2
分子量：542.68
溶解度:DMSO: 250 mg/mL (460.68 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

BI-4020 is a fourth-generation, orally active, and non-covalent EGFR tyrosine kinase inhibitor, which 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) whilst sparing activity against EGFR wt (IC50=190 nM). BI-4020 shows high kinome selectivity and good DMPK properties[1].

BI-4020 inhibits p-EGFR del19 T790M C797S with an IC50 of 0.6 nM[1].

BI-4020 leads to tumor regressions in the human PC-9 (EGFR del19 T790M C797S) triple mutant NSCLC xenograft model in mice[1].

[1]. Engelhardt H,et al. Start selective and rigidify: The discovery path towards a next generation of EGFR tyrosine kinase inhibitors. J Med Chem. 2019 Nov 5.