JNJ-38877605 |
Catalog No.GC12585 |
JNJ-38877605는 4nM의 IC50을 가진 c-Met의 ATP 경쟁적 억제제이며, 200개의 다른 티로신 및 세린-트레오닌 키나제보다 c-Met에 대해 600배 선택적입니다.
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Cas No.: 943540-75-8
Sample solution is provided at 25 µL, 10mM.
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 [1].
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 [2].
Clinical trial: A Safety and Dose-finding Study of JNJ-38877605 in Patients With Advanced or Refractory Solid Tumors.
Reference:
[1] 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;
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