Sunvozertinib 是一种有效的ErbBs(EGFR、HER2，尤其是突变型) 和BTK抑制剂。Sunvozertinib 显示 EGFR 外显子 20 NPH 插入、EGFR 外显子 20 ASV 插入、EGFR L858R 和 T790M 突变以及 HER2 外显子 20 YVMA 和 EGFR WT A431 的IC50分别为 20.4、20.4、1.1、7.5 和 80.4 nM (详细信息请参考专利 WO2019149164A1, example 52)。

Sunvozertinib is a potent ErbBs (EGFR, Her2, especially mutant forms) and BTK inhibitor. Sunvozertinib shows IC 50 s of 20.4, 20.4, 1.1, 7.5, and 80.4 nM for EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively (patent WO2019149164A1, example 52) [1].

Sunvozertinib shows GI 50 s of 60.4, 83.2, 3.3, 101.3, and 47.1 nM for EGFR exon NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively. Sunvozertinib shows GI 50 s of 3.2, 5.8, 51.3, and 1983.5 nM for BTK WT OCI-LY-10, BTK WT TMD-8, BTK WT Ri-1, and non-BCR activated DB, respectively [1]. Sunvozertinib inhibits p-BTK with IC 50 of 1.6 nM [1].

2370013-12-8

C29H35ClFN7O3

584.08

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years