SIAIS164018 hydrochloride is a PROTAC-based degrader targeting ALK and EGFR, exhibiting IC50 values of 2.5 nM for ALK and 6.6 nM for ALK G1202R. It effectively suppresses cancer cell migration and invasion, induces G1 cell cycle arrest, and promotes apoptosis, demonstrating superior properties compared to Brigatinib [1].

SIAIS164018 hydrochloride（0-1 μM；16小时）显著抑制SR细胞增殖[1]。在0-100 nM浓度和72小时处理时间下，SIAIS164018 hydrochloride对于过表达ALK (G1202R)的293T细胞和表达EGFR的H1975细胞系展现出超过Brigatinib的细胞增殖抑制效果[1]。100 nM浓度下，SIAIS164018 hydrochloride可在24或48小时内在ALK阴性的Calu-1和MDA-MB-231细胞线中诱导明显的G1期细胞周期阻滞[1]。浓度范围在0.01-1000 nM，处理时间为16小时的SIAIS164018 hydrochloride能够下调ALK阳性的SR细胞系和ALK阴性的Calu-1细胞系中的FAK、PYK2、FER、RSK1以及GAK的蛋白表达水平[1]。