JNJ-38877605 is a small-molecule ATP-competitive inhibitor of the catalytic activity of c-Met.
Extensive evidence that c-Met signaling is involved in the progression and spread of several cancers and an enhanced understanding of its role in disease have generated considerable interest in c-Met and HGF asmajor targets in anti-cancer drug development.
In vitro: JNJ-38877605 showed ~600-fold selectivity for c-Met compared with a panel of ~250 diverse tyrosine and serine-threonine kinases and was found to potently inhibit HGF-stimulated and constitutively activated c-Met phosphorylation in vitro .
In vivo: JNJ-38877605 showed excellent oral bioavailability approaching 100% in all examined species. In addition, JNJ-38877605 in a single dose was observed toinhibit Met phosphorylation in tumor xenografts for up to16 h. Inhibition of Met phosphorylation was associated withdose-dependent tumor growth inhibition using a range of oral dosing regimens .
Clinical trial: A Safety and Dose-finding Study of JNJ-38877605 in Patients With Advanced or Refractory Solid Tumors.
 PereraT, L avrijssenT, Janssens B, et al. JNJ-38877605: a selective Met kinase inhibitor inducing
regression of Met-driven tumor models. Presented at the 99th AACR Annual Meeting; 2008 Apr 12 -16;
|Storage||Store at -20°C|
|Solubility||≥18.85mg/mL in DMSO|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
|Description||JNJ-38877605 is an ATP-competitive inhibitor of c-Met with an IC50 value of 4 nM.|