alk-in-12

ALK-IN-12 is a highly potent and orally active inhibitor of anaplastic lymphoma kinase (ALK), demonstrating an exceptional IC50 value of 0.18 nM. Additionally, ALK-IN-12 displays inhibitory activity against insulin-like growth factor 1 receptor (IGF1R) and insulin receptor (InsR), with IC50 values of 20.3 nM and 90.6 nM, respectively. Notably, its antitumor effects have been observed, making it a promising compound for targeted cancer therapy.

A 83-01 (ALK5 Inhibitor IV) 是一种 TGF-βI 型受体 ALK5、ALK4 和 ALK7 的抑制剂 (IC50=12 45 7.5 nM)。A 83-01 可促进小鼠成纤维细胞重编程为 iPSCs。A 83-01 可用于类器官培养。

ALK-IN-9 (compound 40) is a highly effective ALK inhibitor. It demonstrates remarkable inhibitory activity against cell proliferation, with IC50 values of <0.2 nM for Ba F3-EML4-ALK, KM 12 (TPM3-TRKA), and KG-l cell (OP2-FGFR1).

SIAIS039是一款针对c-ros致癌基因1(ROS1)的口服活性PROTAC,它在HCC78细胞、Ba F3细胞(表达CD74-ROS1融合)以及Ba F3细胞(表达SDC4-ROS1融合)中展现出的DC50分别为154.46 nM、126.47 nM、143.69 nM.该化合物能够抑制ROS1阳性细胞的增殖、诱导细胞周期停滞和细胞凋亡,并有效抑制克隆形成.在动物体内试验中,SIAIS039也显示出了对ROS1驱动型肿瘤生长的明显抑制效果.SIAIS039的组成包括ALK抑制剂Brigatinib、连接子EM-12以及VHL E3泛素连接酶配体。