Product Overview
Entrectinib | T3678 | TargetMol Chemicals
CAS: 1108743-60-7
Smiles: CN1CCN(CC1)c1ccc(C(=O)Nc2n[nH]c3ccc(Cc4cc(F)cc(F)c4)cc23)c(NC2CCOCC2)c1
Formula: C31H34F2N6O2
Pathway: Angiogenesis|||Autophagy|||Immunology/Inflammation|||Tyrosine Kinase/Adaptors
Target: Trk receptor|||ROS|||ALK|||Autophagy
Receptor: N/A
Bioactivity: Entrectinib is an inhibitor of TrkA (IC50: 1.7 nM), TrkB (IC50: 0.1 nM), and TrkC (IC50: 0.1 nM), as well as anaplastic lymphoma kinase (ALK; IC50: 1.6 nM) and C-ros oncogene 1 (ROS1; IC50: 0.2 nM). Entrectinib blocks proliferation of ALK-dependent cell lines, including those with C1156Y or L1196M resistance mutations, and inhibits ALK‐dependent signaling. It has been shown to inhibit the growth of a non-small cell lung Y cell line bearing an EML4-ALK rearrangement. In mice bearing various ROS1, Trk, or ALK-driven xenografts, Entrectinib has been shown to induce tumor regression.
Molecular Weight: 560, 65
