产品描述:
Entrectinib is an inhibitor of TrkA (IC50 = 1.7 nM), TrkB (IC50 = 0.1 nM), and TrkC (IC50 = 0.1 nM), as well as C-ros oncogene 1 (ROS1; IC50 = 0.2 nM) and anaplastic lymphoma kinase (ALK; IC50 = 1.6 nM).{31678,31677} Entrectinib blocks proliferation of ALK-dependent cell lines, including those with L1196M or C1156Y resistance mutations, and inhibits ALK‐dependent signaling.{31677,31679} It has been shown to inhibit the growth of a non-small cell lung cancer cell line bearing an EML4-ALK rearrangement.{31677,31679} In mice bearing various Trk, ROS1, or ALK-driven xenografts, entrectinib has been shown to induce tumor regression.{31677,31679}