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Chemical Structure| 881202-45-5 同义名 : JNJ-26854165
CAS号 : 881202-45-5
货号 : A603239
分子式 : C21H20N4
纯度 : 99%+
分子量 : 328.41
MDL号 : MFCD16620518
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -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
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].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 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
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 - -
实验方案
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
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.