CAS: 1802220-02-5

(7S,13R)-11-Fluoro-6,7,13,14-Tetrahydro-7,13-Dimethyl-1,15-Etheno-1H-Pyrazolo[4,3-f][1,4,8,10]Benzoxatriazacyclotridecin-4(5H)-One

Repotrectinib

Repotrectinib (TPX-0005) is a potent ALK/ROS1/TRK inhibitor, with IC50 of 1.01/5.3/1.08/1.26 nM for WT ALK, SRC, ALK L1196M and ALK G1202R, respectively.

Repotrectinib is an inhibitor of the enzyme c-Met, which is a receptor tyrosine kinase that is involved in various cellular processes. It has been shown to have potent antitumor activity against many solid tumor cell lines and murine xenografts. Repotrectinib inhibits cancer cells by binding to the c-Met receptor and preventing it from initiating downstream signaling pathways. The drug also has a low expression in normal tissues, which limits its toxicity. Repotrectinib's mechanism of action is through inhibition of the protein secretase, which prevents the conversion of pro-caspase-1 into active caspase-1. Caspase-1 has been shown to be essential for apoptosis induction in cancer cells.