UNC2250 is a potent and selective Mer inhibitor with an IC50 of 1.7 nM, about 160- and 60-fold selectivity over the closely related kinases Axl/Tyro3.
体外研究
UNC2250 (5-500 nM; 1 hour) inhibits Mer phosphorylation in 697 B-ALL cells with an IC50 value of 9.8 nM.
UNC2250 efficiently inhibits ligand-dependent phosphorylation of a chimeric protein consisting of the extracellular and transmembrane domains of the epidermal growth factor (EGF) receptor and the intracellular tyrosine kinase domain of Mer.
UNC2250 incubation inhibits colony formation in soft agar cultures of the BT-12 rhabdoid tumor and the Colo699 NSCLC cell lines .
Western Blot Analysis
Cell Line:
697 B-ALL cells
Concentration:
5, 10, 20, 50, 100, 250, 500 nM
Incubation Time:
1 hour
Result:
Inhibits Mer phosphorylation in 697 B-ALL cells with an IC50 value of 9.8 nM.
分子式
C24H36N6O2
分子量
440.58
CAS号
1493694-70-4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO : 20 mg/mL (45.39 mM; ultrasonic and warming and heat to 60°C)
0.1 M HCL : 12.5 mg/mL (28.37 mM; ultrasonic and adjust pH to 3 with HCl)