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).

Entrectinib-d4 是 Paquinimod 的氘代标记同位素。Entrectinib 是一种口服有效的 TrkA/B/C、ROS1 和 ALK 抑制剂，能够穿透血脑屏障并具有中枢神经系统活性，其 IC50 值分别为 1 nM、3 nM、5 nM、12 nM 和 7 nM。它可以诱导癌细胞凋亡和阻止细胞周期，展现出强劲的抗肿瘤活性，还能减轻博来霉素引起的小鼠肺纤维化。

Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) 是一种氘代形式的Entrectinib。Entrectinib (NMS-E628) 是一种有效的口服制剂，能够透过血脑屏障并作用于中枢神经系统，作为TrkA/B/C、ROS1和ALK的抑制剂，其IC50值分别为1, 3, 5, 12和7 nM。Entrectinib 可以诱导癌细胞凋亡和细胞周期停滞，展现良好的抗肿瘤活性，并能减轻由博来霉素引起的小鼠肺纤维化。