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Serdemetan {[allProObj[0].p_purity_real_show]}

货号:A603239 同义名: JNJ-26854165 Ambeed 开学季,买赠积分,赢豪礼

Serdemetan acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, and inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53.

Serdemetan 化学结构 CAS号:881202-45-5
Serdemetan 化学结构
CAS号:881202-45-5
Serdemetan 3D分子结构
CAS号:881202-45-5
Serdemetan 化学结构 CAS号:881202-45-5
Serdemetan 3D分子结构 CAS号:881202-45-5
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Serdemetan 纯度/质量文件 产品仅供科研

货号:A603239 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

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产品名称 p53 其他靶点 纯度
Pifithrin-μ {[allProObj[0].p_purity_real_show]}
Pifithrin-α HBr {[allProObj[0].p_purity_real_show]}
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Serdemetan 生物活性

靶点
  • E3 Ligase

描述 JNJ-26854165 is a p53-activating agent which can induce p53-mediated apoptosis in acute leukemia cells with wild-type p53, in which p53 rapidly drives transcription-independent apoptosis followed by activation of a transcription-dependent pathway. It accelerated the proteasome-mediated degradation of p21 and antagonized the transcriptional induction of p21 by p53[3]. The action of JNJ-26854165 relies on HDM2, a key regulator of p53, mediating its rapid degradation. It is regarded as a first-in-class HDM2-inhibitor in phase I development[2].

Serdemetan 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
5637 cell Growth inhibition assay Inhibition of human 5637 cell growth in a cell viability assay, IC50=4.79652 μM SANGER
769-P cell Growth inhibition assay Inhibition of human 769-P cell growth in a cell viability assay, IC50=1.82224 μM SANGER
786-0 cell Growth inhibition assay Inhibition of human 786-0 cell growth in a cell viability assay, IC50=1.72989 μM SANGER
AGS cell Growth inhibition assay Inhibition of human AGS cell growth in a cell viability assay, IC50=5.47711 μM SANGER

Serdemetan 动物研究

Dose Mice: 20 mg/kg[3] (p.o.), 50 mg/kg[4] (p.o.)
Administration p.o.

Serdemetan 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00676910 Neoplasms Phase 1 Completed - -

Serdemetan 参考文献

[1]Kojima K, Burks JK, et al. 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.

[2]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

[3]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. doi: 10.1158/1535-7163.MCT-10-0337. Epub 2010 Aug 24. PMID: 20736344; PMCID: PMC2949269.

Serdemetan 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.04mL

0.61mL

0.30mL

15.22mL

3.04mL

1.52mL

30.45mL

6.09mL

3.04mL

Serdemetan 技术信息

CAS号881202-45-5
分子式C21H20N4
分子量 328.41
别名 JNJ-26854165
运输蓝冰
存储条件

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 50 mg/mL(152.25 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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