Molecular Formula | C29H28N6O2 |
Molar Mass | 492.57 |
Density | 1.25 |
Boling Point | 626.5±65.0 °C(Predicted) |
pKa | 8.93±0.10(Predicted) |
Storage Condition | -20℃ |
In vitro study | EMD 1214063 inhibited HGF-induced phosphorylation in A549 cells by c-Met with an IC50 of 6 nM. EMD 1214063 treatment induced a significant reduction in phosphorylation of EBC-1 components in c-Met cells with an IC50 of 9 nM. EMD 1214063 effectively blocks the phosphorylation of major downstream effector proteins of c-Met enzymes, such as Grb2,Gab1,Sos,PLC gamma, and phosphatidylinositol 3-kinase, in EBC-1,MKN-45, and Hs746T cells, range from 1 to 10 nM. EMD 1214063 greatly inhibited the activity of MKN-45 cells, IC50 less than 1 nM. Treatment with EMD 1214063 (0.1 nM) inhibited HGF-induced NCI-H441 cell migration, whereas concentrations from 100 nM to 1 μm inhibited it almost completely. EMD 1214063 inhibited HGF-induced phosphorylation in A549 cells by c-Met with IC50 of 6 nM. EMD 1214063 treatment induced a significant reduction in phosphorylation of EBC-1 components in c-Met cells with an IC50 of 9 nM. EMD 1214063 effectively blocks the phosphorylation of major downstream effector proteins of c-Met enzymes, such as Grb2,Gab1,Sos,PLC gamma, and phosphatidylinositol 3-kinase, in EBC-1,MKN-45, and Hs746T cells, range from 1 to 10 nM. EMD 1214063 greatly inhibited the activity of MKN-45 cells, IC50 less than 1 nM. Treatment with EMD 1214063 (0.1 nM) inhibited HGF-induced NCI-H441 cell migration, whereas concentrations from 100 nM to 1 μm inhibited it almost completely. |
In vivo study | Treatment of EMD 1214063 at a dose of 10 mg/kg or higher resulted in inhibition of c-Met phosphorylation in more than 90% of Hs746T xenograft tumors for at least 72 hours. EMD 1214063 induced a greater than 50% reduction in the expression of cyclin D1 and this effect persisted for more than 96 hours at a dose of 100 mg/kg. Transient p27 sensing and cleavage of caspase-3 was also observed after EMD 1214063 treatment. EMD 1214063 (15 mg/kg per day) treatment induced c-Met amplification, overexpression, and complete regression of gastric cancer xenograft Hs746T activated in a ligand-independent manner. EMD 1214063 treatment at a dose of 10 mg/kg or higher resulted in inhibition of c-Met phosphorylation in more than 90% of Hs746T xenograft tumors for at least 72 hours. EMD 1214063 induced a greater than 50% reduction in the expression of cyclin D1 and this effect persisted for more than 96 hours at a dose of 100 mg/kg. Transient p27 sensing and cleavage of caspase-3 was also observed after EMD 1214063 treatment. EMD 1214063 (15 mg/kg per day) treatment induced c-Met amplification, overexpression, and complete regression of gastric cancer xenograft Hs746T activated in a ligand-independent manner. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.03 ml | 10.151 ml | 20.302 ml |
5 mM | 0.406 ml | 2.03 ml | 4.06 ml |
10 mM | 0.203 ml | 1.015 ml | 2.03 ml |
5 mM | 0.041 ml | 0.203 ml | 0.406 ml |