AP26113

Ферментативный ингибитор

This potent ALK inhibitor (FW = 529.02 g/mol; CAS 1197958-12-5; Solubility: 45 mg/mL DMSO; <1 mg/mL H2O), also named 5-chloro-N2-[4-[4-(dimethylamino)-1-piperidinyl]-2-methoxyphenyl]-N4-[2-(dimethyl- phosphinyl)phenyl]-2,4-pyrimidinediamine, inhibits wild type Lymphoma Kinase, or ALK (Ki = 0.62 nM) and overcomes crizotinib resistance in non- small cell lung cancers harboring the fusion oncogene EML4-ALK. Cells often develop the L1196M gatekeeper mutation within the kinase domain, a changes that renders them resistant to crizotinib, even at higher drug doses (1 μM). AP26113 is highly active against these resistant cancer cells, both in vitro and in vivo.