| 产品描述: | Mertk 抑制剂;Mertk Inhibitors;;InformationUNC2250 UNC2250 is a potent and selective Mer inhibitor with IC50 of 1.7 nM, about 160- and 60-fold selectivity over the closely related kinases Axl/Tyro3.TargetsAxl ; Axl ; Mer ; Tyro3 ; 1.7 nM; 100 nMIn vitroUNC2250 efficiently inhibits Mer phosphorylation in 697 B-ALL cells and Colo699 NSCLC cells. Moreover, UNC2250 also displays functional antitumor activity by reducing colony-forming potential in both rhabdoid tumor cells and NSCLC cells.In vivoAccording to in vivo PK experiment, UNC2250 has a moderate half-life, clearance, and volume of distribution as well as reasonable oral bioavailability and good solubility.Cell Research(from reference)Cell lines:BT-12 rhabdoid tumor cells, and Colo699 NSCLC cells Concentrations:~3 μM for BT-12, ~300 nM for Colo699 Incubation Time:3 weeks for BT-12, 2 weeks for Colo699 |