Serdemetan(JNJ-26854165)是HDM2泛素连接酶拮抗剂，能诱导p53野生型细胞的早期凋亡。

Serdemetan(JNJ-26854165) 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. IC50 value: HDM2 ubiquitin ligase Target: in vitro: JNJ 26854165 is a novel tryptamine derivative which activates p53 and acts as a HDM2 ubiquitin ligase antagonist. JNJ 26854165 inhibits cell growth and induces apoptosis in leukemia cell lines with IC50 values of 0.24, 0.33, 0.32 and 0.44 μM at 72 hours for OCI-AML-3, MOLM-13, NALM-6 and REH cells, respectively. In addition, JNJ 26854165 accelerates proteasome-mediated degradation of p21 and antagonizes the transcriptional induction of p21 by p53. It also induces S-phase delay and upregulates E2F1 expression in p53 mutant cells, resulting in preferential apoptosis of S-phase cells. JNJ 268

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Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 50 mg/mL (152.25 mM; Need ultrasonic)配制储备液