- Product NameEntrectinib
- Brief DescriptionInhibitors
- Purification99.49%
- Biological ActivityEntrectinib 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). Entrectinib blocks proliferation of ALK-dependent cell lines, including those with L1196M or C1156Y 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 Trk, ROS1, or ALK-driven xenografts, entrectinib has been shown to induce tumor regression.
- Target NameALK inhibitor; ROS inhibitor; Trk receptor inhibitor
- CAS No. 1108743-60-7
- Calculated MW 560.64
- Formulation C31H34F2N6O2
- Storage 3 years -20˚C powder;2 years -80˚C in solvent;
