PLX51107

PLX51107 is a potent and selective BET inhibitor, with Kds 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 also interacts with the bromodomains of CBP and EP300 (Kd, in the 100 nM range) .

Product Specifications

CAS Number

[1627929-55-8]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Epigenetic Reader Domain

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/PLX51107.html

Purity

99.98

Solubility

DMSO : 75 mg/mL (ultrasonic)

Smiles

C[C@@H](C1=NC=CC=C1)N2C=C(C3=CC=C(C(O)=O)C=C3)C4=NC=C(C5=C(C)ON=C5C)C=C42

Molecular Formula

C26H22N4O3

Molecular Weight

438.48

Precautions

H302, H315, H319, H335

References & Citations

[1]Ozer HG, 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 Apr;8 (4) :458-477.