JNJ-26854165 (Serdemetan) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53.
Cat.No
DC7175
Name
JNJ-26854165 (Serdemetan)
Chemical Properties
CAS
881202-45-5
Formula
C21H20N4
MW
328.4103
Storage
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
References
[1]. T. Stühmer et al. A first-in-class HDM2-inhibitor (JNJ-26854165) in phase I development shows potent activity against multiple myeloma (MM) cells in vitro and ex vivo Journal of Clinical Oncology, 2008 ASCO Annual Meeting Proceedings (Post-Meeting Edition ).Vol 26, No 15S (May 20 Supplement), 2008: 14694
[2]. Chargari C, Leteur C, Angevin E, Bashir T, Schoentjes B, Arts J, Janicot M, Bourhis J, Deutsch E.Preclinical assessment of JNJ-26854165 (Serdemetan), a novel tryptamine compound with radiosensitizing activity in vitro and in tumor xenografts.Cancer Lett. 2011 Dec 22;312(2):209-18.
[3]. Smith MA, Gorlick R, Kolb EA, Lock R, Carol H, Maris JM, Keir ST, Morton CL, Reynolds CP, Kang MH, Arts J, Bashir T, Janicot M, Kurmasheva RT, Houghton PJ.Initial testing of JNJ-26854165 (Serdemetan) by the pediatric preclinical testing program.Pediatr Blood Cancer. 2012 Aug;59(2):329-32.
[4]. Tabernero J, Dirix L, Sch?ffski P, Cervantes A, Lopez-Martin JA, Capdevila J, van Beijsterveldt L, Platero S, Hall B, Yuan Z, Knoblauch R, Zhuang SH.A phase I first-in-human pharmacokinetic and pharmacodynamic study of serdemetan in patients with advanced solid tumors.Clin Cancer Res. 2011 Oct 1;17(19):6313-21. Epub 2011 Aug 10.
[5]. Kojima K, Burks JK, Arts J, Andreeff M.The novel tryptamine derivative JNJ-26854165 induces wild-type p53- and E2F1-mediated apoptosis in acute myeloid and lymphoid leukemias.Mol Cancer Ther. 2010 Sep;9(9):2545-57. Epub 2010 Aug 24.
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