Samuraciclib hydrochloride (ICEC0942 hydrochloride) is a potent, selective, ATP competitive and oral active CDK7 inhibitor with IC50 of 41 nM. The selectivity of Samuraciclib hydrochloride is 45-, 15-, 230- and 30-fold higher than CDK1, CDK2 (IC50 is 578 nM), CDK5 and CDK9 respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride has anti-tumor effects.

CDK6-CyclinD1:34 μM, CDK4-CyclinD1:49 μM, CDK9-CyclinT1:1.2 μM, CDK7-CyclinH:41 nM, CDK2-CyclinA:578 nM, CDK5-p35 NCK:9.4 μM, CDK1-CyclinA:1.8 μM

Samuraciclib（ICEC0942；0-10 μM；24小时；HCT116细胞）处理能促进细胞凋亡，并引起细胞周期阻滞。该化合物在剂量和时间依赖性方式内抑制HCT116结肠癌细胞中PolII CTD的磷酸化，并阻断CDK1、CDK2以及视网膜母细胞瘤蛋白的磷酸化。Samuraciclib（ICEC0942）对MCF7、T47D、MDA-MB-231、HS578T、MDA-MB-468、MCF10A及HMEC细胞的生长抑制具有GI50值分别为0.18 μM、0.32 μM、0.33 μM、0.21 μM、0.22 μM、0.67 μM及1.25 μM。

Samuraciclib（ICEC0942；100 mg/kg；口服管饲；每日一次；连续14天；雌性nu/nu-BALB/c无胸腺裸鼠）治疗在第14天抑制60%的肿瘤体积增长，抑制外周血单核细胞（PBMC）及肿瘤中PolII Ser2和Ser5的磷酸化。Samuraciclib（ICEC0942）与ICI 47699联合治疗显示了雌激素受体（ER）阳性肿瘤异种移植物的完全停滞。