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) is an inhibitor of the TGF-β type I receptors ALK5, ALK4, and ALK7 (IC50=12 45 7.5 nM). A 83-01 promotes the reprogramming of mouse fibroblasts into iPSCs. A 83-01 can be used in organoid cultures.

ALK-IN-9 (compound 40) is a highly effective ALK inhibitor, demonstrating remarkable inhibitory activity against cell proliferation, with IC50 values of <0.2 nM for Ba F3-EML4-ALK, KM 12 (TPM3-TRKA), and KG-1 cell (OP2-FGFR1).

SIAIS039 is an orally active PROTAC specifically targeting c-ros oncogene 1 (ROS1), demonstrating DC50 values of 154.46 nM, 126.47 nM, and 143.69 nM in HCC78 cells, Ba F3 cells expressing CD74-ROS1 fusion, and Ba F3 cells expressing SDC4-ROS1 fusion, respectively. This compound inhibits proliferation, induces cell cycle arrest, and triggers apoptosis in ROS1-positive cells, while also inhibiting colony formation. In vivo, SIAIS039 exhibits potent anti-tumoral activity against ROS1-driven tumor growth. The composition of SIAIS039 includes the ALK inhibitor Brigatinib, linker EM-12, and VHL E3 ubiquitin ligase ligand.