Name: JNJ-26854165 (Serdemetan)
Price: 260.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    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:
    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
    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.
- Properties
  - Categories
    
    P53 activator, blocking Mdm2-p53 interaction
    
    Alternative Name
    
    JNJ 26854165; 1-N-[2-(1H-indol-3-yl)ethyl]-4-N-pyridin-4-ylbenzene-1,4-diamine
    
    CAS Number
    
    881202-45-5
    
    Molecular Formula
    
    C21H20N4
    
    Molecular Weight
    
    328.41
    
    Appearance
    
    A solid
    
    Purity
    
    98.35%
    
    Solubility
    
    insoluble in EtOH; insoluble in H2O; ≥14.8 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    C1=CC=C2C(=C1)C(=CN2)CCNC3=CC=C(C=C3)NC4=CC=NC=C4
    
    * For Research Use Only
- Reference
  - 1. Chen R, Zhou J, et al. "A Fusion Protein of the p53 Transaction Domain and the p53-Binding Domain of the Oncoprotein MdmX as an Efficient System for High-Throughput Screening of MdmX Inhibitors." Biochemistry. 2017 Jun 27;56(25):3273-3282. PMID:28581721