PLX51107 | BET Inhibitor | AmBeed-信号通路专用抑制剂

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PLX51107 99%+

货号：A714146

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.

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： 99%+ 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

表观遗传阅读框亚型比较

产品名称	BET ↓ ↑	bromodomain ↓ ↑	BRPF ↓ ↑	CBP/beta-catenin ↓ ↑	p300/CBP ↓ ↑	其他靶点	纯度
MS436	++ BRD4 (1), Ki: <0.085 μM BRD4 (2), Ki: 0.34 μM						99%+
CPI-203	+++ BRD4, IC50: 37 nM						99+%
GSK1324726A	+++ BRD2, IC50: 31 nM BRD4, IC50: 22 nM						99%+
PFI-1	++ BRD2, IC50: 98 nM BRD4, IC50: 0.22 μM						98%
Apabetalone	+ BD2, IC50: 0.51 μM						99%
(+)-JQ1	+++ BRD4 (2), IC50: 33 nM BRD4 (1), IC50: 77 nM						98%
I-BET151	+ BRD3, IC50: 0.25 μM BRD4, IC50: 0.5 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						99+%
Pelabresib	+++ BRD4-BD1, IC50: 39 nM						98%
ARV-825	+++ BRD4 BD1, Kd: 90 nM BRD4 BD2, Kd: 28 nM						99%+
Birabresib							99%+
BI 2536	+++ BRD4, Kd: 37 nM					c-Myc	99%+
Bromosporine	++ BRD2, IC50: 0.29 μM BRD9, IC50: 0.122 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	++++ Brd3(BD2), Kd: 13 nM Brd2(BD2), Kd: 62 nM						99%+
dBET57	+ BRD4_BD1, DC50: 500 nM						99%+
SF2523	+ BRD4, IC50: 241 nM					DNA-PK	99%+
INCB054329	++++ BRD3-BD1, IC50: 9 nM BRD4-BD1, IC50: 119 nM						99%
INCB-057643	✔						99%+
(E/Z)-ZL0420	+++ BRD4 BD2, IC50: 32 nM BRD4 BD1, IC50: 27 nM						99%+
BMS-986158	✔						99%+
BRD4 Inhibitor-10	++++ BRD4-BD2, IC50: 41 nM BRD4-BD1, IC50: 5 nM						97%
A1874	✔						99%+
Y06036	++ BRD4 (1), Kd: 82 nM						99%+
Alobresib	✔					NF-κB	98%
ODM-207	✔						99%
GSK778	+++ BRD4-BD1, IC50: 143 nM BRD2-BD1, IC50: 75nM						97%
SRX3207	+ BRD42, IC50: 3070 nM BRD41, IC50: 3070 nM					Syk	98%
GSK046	+++ BRD4_BD2, IC50: 214 nM BRD3_BD2, IC50: 98 nM						98%
GSK620	✔						97%
Thalidomide-NH-C4-NH-Boc	✔						98%
Trotabresib	✔						99%
NHWD-870	✔						98%
CFT8634	++++ BRD9, DC50: 3 nM						98%
GSK2801		++ BAZ2A, Kd: 257 nM BAZ2B, Kd: 136 nM					99%+
KG-501		✔					99%+
UNC 669		+ L3MBTL4, IC50: 6 μM L3MBTL3, IC50: 35 μM					98%
PFI-3		+++ SMARCA2A, Kd: 72 nM SMARCA4, Kd: 55 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			++ BRPF1B, Kd: 100 nM BRPF2, Kd: 500 nM				99%+
GSK-5959			++ BRPF3, pIC50: 7.1 BRPF2, pIC50: 5.2				99%
GSK6853			++++ BRPF1, pIC50: 8.1				99%+
NI-42			++++ BRPF1, IC50: 48 nM BRPF3, IC50: 260 nM				99%+
E-7386				+++ CBP/beta-catenin, IC50: 0.0484 μM			97%
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					+ PCAF, IC50: 5 μM p300/CBP, IC50: 8.5 μM		99%+
SGC-CBP30					++++ CREBBP, IC50: 21 nM EP300, IC50: 38 nM		99%+
Nordihydroguaiaretic acid					✔	HER2,IGF-1R	99%+
Curcumin					+ p300, IC50: ~25 μM	NF-κB,Ferroptosis,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		98%
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

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

PLX51107 99%+

PLX51107 纯度/质量文件产品仅供科研

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PLX51107 99%+

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全球学术期刊中引用的产品

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PLX51107 生物活性

PLX51107 临床研究

PLX51107 参考文献

PLX51107 实验方案

PLX51107 技术信息

最近浏览的产品

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