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.
Storage Temp
Store at -80°C
Shipped In
Ice chest + Ice pads
Product Description
Information
UNC2250 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.
Targets
Axl ; Axl ; Mer ; Tyro3 ; 1.7 nM; 100 nM
In vitro
UNC2250 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 vivo
According 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
