P53 activator, blocking Mdm2-p53 interaction
CAS：881202-45-5
分子式：C21H20N4
分子量：328.41
纯度：98%
存储：Store at -20°C

Background:

JNJ-26854165, also named as Serdemetan, is originally developed as an activator of p53, is now regarded as a novel oral Human Double Minute-2 (HDM-2) ubiquitin ligase antagonist. It can increase the level of HDM-2 client proteins, such as p53, by inhibiting the association of HDM-2-client protein complex with the proteosome. It is demonstrated potent anti-proliferative and apoptosis-inducing activity of JNJ-26854165 in a broad range of p53 wild type and mutant tumor models. In vivo, JNJ-26854165 may induce important differences in EFS distribution when comparing to control in 18 of 37 solid tumors and in 5 of 7 of the evaluable ALL xenografts.

Reference

[1].J. Tabernero, L. Dirix, P. Schoffski, A. Cervantes, J. Capdevila, J. Baselga, L. van Beijsterveldt, H. Winkler, S. Kraljevic and S. H. Zhuang. Phase I pharmacokinetic (PK) and pharmacodynamic (PD) study of HDM-2 antagonist JNJ-26854165 in patients with advanced refractory solid tumors. Journal of Clinical Oncology (Meeting Abstracts) May 2009 vol. 27 no. 15S 3514
[2].Malcolm A. Smith, Richard Gorlick, E. Anders Kolb, Richard Lock, Hernan Carol, John M. Maris, Stephen T. Keir, Christopher L. Morton, C. Patrick Reynolds, Min H. Kang, Janine Arts, Tarig Bashir, Michel Janicot, Raushan T. Kurmasheva, Peter J. Houghton. Initial testing of JNJ-26854165 (Serdemetan) by the pediatric preclinical testing program. Pediatric Blood & Cancer. Volume 59, Issue 2, pages 329–332, August 2012.