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).

Entrectinib-d4 is the deuterium-labeled isotope of Paquinimod. Entrectinib is an orally active inhibitor of TrkA/B/C, ROS1, and ALK, capable of crossing the blood-brain barrier and possessing central nervous system activity, with IC50 values of 1, 3, 5, 12, and 7 nM, respectively. It induces apoptosis and cell cycle arrest in cancer cells, exhibits antitumor efficacy, and mitigates bleomycin-induced pulmonary fibrosis in mice.

Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is the deuterated form of Entrectinib. Entrectinib (NMS-E628) is an orally bioavailable inhibitor that effectively crosses the blood-brain barrier and exhibits central nervous system activity. It targets TrkA/B/C, ROS1, and ALK with IC50 values of 1, 3, 5, 12, and 7 nM, respectively. Entrectinib induces apoptosis and cell cycle arrest in cancer cells, demonstrates antitumor properties, and alleviates bleomycin-induced pulmonary fibrosis in mice.