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PLX51107

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Chemical Structure| 1627929-55-8 同义名 : -
CAS号 : 1627929-55-8
货号 : A714146
分子式 : C26H22N4O3
纯度 : 99%+
分子量 : 438.478
MDL号 : MFCD31657388
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 80 mg/mL(182.45 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：
生物活性
靶点

  • BET

    BRD4 BD2, Kd:1.7 nM

    BRD3 BD1, Kd:2.1 nM
描述 The BET (bromodomain and extra terminal) family of proteins, BRD2, BRD3, BRD4 and BRDT, are chromatin readers that regulate transcription of genes by binding to acetylated lysine residues on tails of histones in chromatin[1]. PLX51107 is a potent and selective BET inhibitor, with Kd values of 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1, and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively. PLX51107 prevented CpG-induced cell proliferation in primary Chronic lymphocytic leukemia (CLL) cells in a dose dependent fashion under both continuous and washout conditions. Oral gavage of PLX51107 (20 mg/kg daily) for eight days in mouse model of CLL significantly reduced leukemic disease burden in peripheral blood and spleen with modulation of BRD4 targets, compared to vehicle-treated mice[2]. In mice bearing UM001 xenograft tumors, PLX51107 (90 mg/kg) and AZD4547 (5 mg/kg) alone suppressed tumor size moderately but the combination of PLX51107 and AZD4547 significantly decreased tumor size after 2 weeks of treatment, in comparison with the control[3].
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
NCT02683395 Solid Tumors ... 展开 >>Acute Myeloid Leukemia Myelodysplastic Syndrome Non-Hodgkin's Lymphoma 收起 << Phase 1 Recruiting May 2019 United States, New York ... 展开 >> Columbia University Medical Center Completed New York, New York, United States, 10032 United States, Ohio The Ohio State University Stephanie Spielman Comprehensive Breast Center Recruiting Columbus, Ohio, United States, 43212 United States, Pennsylvania Thomas Jefferson University Completed Philadelphia, Pennsylvania, United States, 19107 United States, South Carolina MUSC/ Hollings Cancer Center Completed Charleston, South Carolina, United States, 29425 United States, Texas South Texas Accelerated Research Therapeutics Completed San Antonio, Texas, United States, 78229 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.28mL

0.46mL

0.23mL

11.40mL

2.28mL

1.14mL

22.81mL

4.56mL

2.28mL
参考文献

[1]Filippakopoulos P, Picaud S, Mangos M, et al. Histone recognition and large-scale structural analysis of the human bromodomain family. Cell. 2012;149(1):214‐231.

[2]Ozer HG, El-Gamal D, Powell B, et al. BRD4 Profiling Identifies Critical Chronic Lymphocytic Leukemia Oncogenic Circuits and Reveals Sensitivity to PLX51107, a Novel Structurally Distinct BET Inhibitor. Cancer Discov. 2018;8(4):458‐477.

[3]Chua V, Orloff M, Teh JL, et al. Stromal fibroblast growth factor 2 reduces the efficacy of bromodomain inhibitors in uveal melanoma. EMBO Mol Med. 2019;11(2):e9081.