PLX51107 |
| Katalog-Nr.GC19298 |
PLX51107 ist ein potenter und selektiver BET-Inhibitor mit Kds von 1,6, 2,1, 1,7 und 5 nM fÜr BD1 und 5,9, 6,2, 6,1 und 120 nM fÜr BD2 von BRD2, BRD3, BRD4 bzw. BRDT; PLX51107 interagiert auch mit den BromodomÄnen von CBP und EP300 (Kd, im Bereich von 100 nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1627929-55-8
Sample solution is provided at 25 µL, 10mM.
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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).
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). PLX51107 (0.156-10 uM) suppresses the CpG-induced proliferation of primary chronic lymphocytic leukemia (CLL) cells. PLX51107 also causes accumulation of p21 and IκBα, reduces c-MYC level, and modulates proapoptotic and antiapoptotic proteins. PLX51107 selectively modulates CLL driver genes[1].
PLX51107 (2 mg/kg, p.o.) inhibits splenomegaly by 75% in the Ba/F3 (murine IL3-dependent pro-B-cell line) splenomegaly mouse model, with the similar effect of 25 mg/kg OTX015. PLX51107 (20 mg/kg, qd, p.o.) exhibits potent antileukemic effects in disease models of aggressive chronic lymphocytic leukemia (CLL) and Richter transformation (RT) via oral administration once daily[1].
References:
[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.
Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)
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