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PLX51107 {[allProObj[0].p_purity_real_show]}

货号:A714146

PLX51107是一种强效且选择性的BRD4抑制剂或BET抑制剂,具有新的体外和体内药理特性,在临床前慢性淋巴细胞白血病模型中,其疗效可以媲美或超过BCR信号通路抑制剂。

PLX51107 化学结构 CAS号:1627929-55-8
PLX51107 化学结构
CAS号:1627929-55-8
PLX51107 3D分子结构
CAS号:1627929-55-8
PLX51107 化学结构 CAS号:1627929-55-8
PLX51107 3D分子结构 CAS号:1627929-55-8
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PLX51107 纯度/质量文件 产品仅供科研

货号:A714146 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 BET bromodomain BRPF CBP/beta-catenin p300/CBP 其他靶点 纯度
MS436 ++

BRD4 (2), Ki: 0.34 μM

BRD4 (1), Ki: <0.085 μM

99%+
CPI-203 +++

BRD4, IC50: 37 nM

98+%
GSK1324726A +++

BRD4, IC50: 22 nM

BRD2, IC50: 31 nM

99%+
PFI-1 ++

BRD4, IC50: 0.22 μM

BRD2, IC50: 98 nM

98%
Apabetalone +

BD2, IC50: 0.51 μM

99%
(+)-JQ1 +++

BRD4 (2), IC50: 33 nM

BRD4 (1), IC50: 77 nM

98%
I-BET151 +

BRD4, IC50: 0.5 μM

BRD3, IC50: 0.25 μM

98%
Molibresib +++

BET proteins, IC50: 35 nM

99%+
I-BRD9 +++

BRD4, pIC50: 5.3

BRD9, pIC50: 7.3

99%+
BI-7273 ++++

BRD9, IC50: 19 nM

BRD7, IC50: 117 nM

97%
Pelabresib +++

BRD4-BD1, IC50: 39 nM

98%
ARV-825 +++

BRD4 BD2, Kd: 28 nM

BRD4 BD1, Kd: 90 nM

99%+
Birabresib 99%+
BI 2536 +++

BRD4, Kd: 37 nM

c-Myc 99%+
Bromosporine ++

BRD9, IC50: 0.122 μM

BRD2, IC50: 0.29 μM

++++

CECR2, IC50: 17 nM

99%+
XMD8-92 ++

BRD4 (1), Kd: 170 nM

99%+
Mivebresib 99%+
BI-9564 ++++

BRD9, Kd: 5.9 nM

BRD7, Kd: 73 nM

++

CECR2, Kd: 77 nM

98%
AZD5153 6-Hydroxy-2-naphthoic acid ++++

FL-BRD4, IC50: 5 nM

99%+
PLX51107 ++++

BRD3 BD1, Kd: 2.1 nM

BRD4 BD2, Kd: 1.7 nM

99%+
FL-411 +

BRD4(1), IC50: 0.43 μM

99%+
ABBV-744 99%+
dBET6 ++++

BRD4, IC50: 14 nM

99%+
dBET1 ++++

BRD4, IC50: 20 nM

99%+
MZ1 ++++

Brd2(BD2), Kd: 62 nM

Brd3(BD2), Kd: 13 nM

99%+
dBET57 +

BRD4BD1, DC50: 500 nM

99%+
SF2523 +

BRD4, IC50: 241 nM

DNA-PK 99%+
INCB054329 ++++

BRD4-BD1, IC50: 119 nM

BRD3-BD1, IC50: 9 nM

99%
INCB-057643 99%+
(E/Z)-ZL0420 +++

BRD4 BD1, IC50: 27 nM

BRD4 BD2, IC50: 32 nM

99%+
BMS-986158 99%+
BRD4 Inhibitor-10 ++++

BRD4-BD1, IC50: 5 nM

BRD4-BD2, IC50: 41 nM

97%
A1874 99%+
Y06036 ++

BRD4 (1), Kd: 82 nM

99%+
Alobresib NF-κB 95%
ODM-207 98%
GSK778 +++

BRD4-BD1, IC50: 143 nM

BRD2-BD1, IC50: 75nM

97%
SRX3207 +

BRD42, IC50: 3070 nM

BRD41, IC50: 3070 nM

Syk 98%
GSK046 +++

BRD3BD2, IC50: 98 nM

BRD4BD2, IC50: 214 nM

98%
GSK620 97%
Thalidomide-NH-C4-NH-Boc 98%
Trotabresib 99%
NHWD-870 98%
CFT8634 ++++

BRD9, DC50: 3 nM

99%
GSK2801 ++

BAZ2B, Kd: 136 nM

BAZ2A, Kd: 257 nM

99%+
KG-501 99%+
UNC 669 +

L3MBTL3, IC50: 35 μM

L3MBTL4, IC50: 6 μM

99%
PFI-3 +++

SMARCA4, Kd: 55 nM

SMARCA2A, Kd: 72 nM

99%+
UNC1215 +++

L3MBTL3, IC50: 120 nM

L3MBTL3- D274A, IC50: 3.5 μM

99%+
EED226 ++

EED, Kd: 82 nM

PRC2, Kd: 114 nM

99%+
BRD9539 98%
UNC926 +

L3MBTL1, Kd: 3.9 μM

99%
666-15 ++

CREB, IC50: 81 nM

99%+
UNC6852 +

EED, IC50: 247 nM

98%
BAZ1A-IN-1 +

BAZ1A, Kd: 0.52 μM

99%+
PFI-4 ++

BRPF2, IC50: 7.9 μM

BRPF1, IC50: 80 nM

99%+
OF-1 ++

BRPF2, Kd: 500 nM

BRPF1B, Kd: 100 nM

99%+
GSK-5959 ++

BRPF2, pIC50: 5.2

BRPF3, pIC50: 7.1

99%
GSK6853 ++++

BRPF1, pIC50: 8.1

99%+
NI-42 ++++

BRPF3, IC50: 260 nM

BRPF1, IC50: 48 nM

99%+
E-7386 +++

CBP/beta-catenin, IC50: 0.0484 μM

99%
I-CBP112 ++

CBP, Kd: 151 nM

p300, Kd: 167 nM

98+%
Histone Acetyltransferase Inhibitor II +

p300, IC50: 5 μM

98%
C646 +

p300/CBP, Ki: 400 nM

99%+
Anacardic Acid +

p300/CBP, IC50: 8.5 μM

PCAF, IC50: 5 μM

99%+
SGC-CBP30 ++++

CREBBP, IC50: 21 nM

EP300, IC50: 38 nM

99%+
Nordihydroguaiaretic acid IGF-1R,HER2 99%+
Curcumin +

p300, IC50: ~25 μM

Ferroptosis,NF-κB,Nrf2 98%
PF-CBP1 HCl ++

CREBBP, IC50: 125nM

p300/CBP, IC50: 363nM

97%
CPI-637 +++

CBP, IC50: 0.03 μM

EP300, IC50: 0.051 μM

99%+
Foscenvivint β-catenin 99%+
A-485 ++

p300 HAT, IC50: 0.06 μM

99%+
GNE-781 +

BRD4(1), IC50: 5100 nM

++++

CBP, IC50: 0.94 nM

99%
NEO2734 +++

BET, IC50: <30 nM

+++

p300/CBP, IC50: <30 nM

99%+
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。

PLX51107 生物活性

靶点
  • BET

    BRD3 BD1, Kd:2.1 nM

    BRD4 BD2, Kd:1.7 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].

PLX51107 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 <<

PLX51107 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.

PLX51107 实验方案

计算器
存储液制备 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

PLX51107 技术信息

CAS号1627929-55-8
分子式C26H22N4O3
分子量 438.478
别名
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere,Room Temperature

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
动物实验配方
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