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CAS No.: 1627929-55-8

PLX51107 Catalog No. CSN21058

Synonyms: PLX51107

PLX51107 is a potent and selective BRD4 inhibitor or BET inhibitor with novel in vitro and in vivo pharmacologic properties that emulates or exceeds the efficacy of BCR signaling agents in preclinical models of CLL.

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实验方案

技术信息

生物活性

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 ... more >>Acute Myeloid Leukemia Myelodysplastic Syndrome Non-Hodgkin's Lymphoma Collapse <<	Phase 1	Recruiting	May 2019	United States, New York ... more >> 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 Collapse <<

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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2806 mL
- 11.4031 mL
- 22.8062 mL
- 5 mM
- 0.4561 mL
- 2.2806 mL
- 4.5612 mL
- 10 mM
- 0.2281 mL
- 1.1403 mL
- 2.2806 mL

技术信息

CAS号

1627929-55-8

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H22N4O3

运输

蓝冰

分子量

438.48

别名

PLX51107

溶解度

DMSO	120.0 mg/mL (273.7 mM)
Water	insoluble

动物实验配方

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