产品描述:
ASP3026 is an inhibitor of anaplastic lymphoma kinase (ALK; IC50s = 3.5, 10, and 5.4 nM for the wild-type, ALKF1174L, and ALKR1275Q enzymes, respectively).{29825} It is selective for ALK over a panel of 86 kinases at 1,000 nM but also inhibits c-Ros oncogene 1 (ROS1) and tyrosine kinase non-receptor 2 (TNK2; IC50s = 8.9 and 5.8 nM, respectively). ASP3026 inhibits the proliferation of Ba/F3 cells expressing nucleophosmin (NPM) or echinoderm microtubule-associated protein-like 4 (ELM4) ALK fusion proteins (IC50s = 84 and 56 nM for NPM-ALK and ELM4-ALK, respectively), as well as several Ba/F3 cells expressing NPM-ALK or ELM4-ALK mutants that are resistant to the c-Met and ALK inhibitor crizotinib (Item No. 12087).{31295} It induces tumor regression in an NCI H2228 non-small cell lung cancer (NSCLC) mouse xenograft model when administered at doses of 10 and 30 mg/kg.{29825}