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概述
JNJ-26854165 (Serdemetan)是一种HDM2泛素连接酶拮抗剂，作用于p53野生型细胞，诱导早期凋亡，在缺乏功能性p53的细胞中，抑制细胞增殖而延迟细胞凋亡。
Information
Serdemetan (JNJ-26854165) 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. Phase
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 26854165 is an oral Mdm2 inhibitor which can inhibit the interaction of Mdm2-p53 complex with the proteasome and increase p53 levels by binding to RING domain of Mdm2. A recent study shows that JNJ 26854165 inhibits clonogenic survival in four human cancer cell lines: H460, A549, p53-WT-HCT116, and p53--HCT116.
In vivo
JNJ 26854165 leads to significant differences in EFS distribution in 17 of the 36 (47%) evaluable solid tumor xenografts and in 5 of 7 (71%) of the evaluable ALL xenografts using a dose of 20 mg/kg administered via oral gavage daily for 5 days, repeated for 6 weeks.
Cell Data
cell lines：
Concentrations：0-10 μM
Incubation Time：72 hours
Powder Purity:≥99%
规格
英文别名
N1-(2-(1H-indol-3-yl)ethyl)-N4-(pyridin-4-yl)benzene-1,4-diamine
规格或纯度
10mM in DMSO
英文名称
Serdemetan (JNJ-26854165)
生化机理
Serdemetan（JNJ-26854165）是一种 HDM2 泛素连接酶拮抗剂，还能诱导 p53 野生型细胞早期凋亡，抑制细胞增殖，并在缺乏功能性 p53 的情况下延迟细胞凋亡。第 1 阶段
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
C1=CC=C2C(=C1)C(=CN2)CCNC3=CC=C(C=C3)NC4=CC=NC=C4
PubChem CID
分子量
328.42
高级数据
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| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 A2311023 |
分析证书 | S408324 |
技术文档和文章
此产品的引用文献
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