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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 binds to the acetylated lysine recognition motifs in the bromodomains of the BRD4 protein, thereby preventing the binding of BRD4 to acetylated lysines on histones. PLX51107 (0.156-10 μM) 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.
In vivo, 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.
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| Animal models | C57BL/6 WT mice |
| Formulation | 10% N-methyl-2-pyrrolidone plus diluent (40% PEG400, 5% TPGS, 5% Poloxamer 407, and 50% water) |
| Dosages | 20 mg/kg, qd (once daily) |
| Administration | oral gavage |
| Molecular Weight | 438.48 |
| Formula | C26H22N4O3 |
| CAS Number | 1627929-55-8 |
| Solubility (25°C) | DMSO: ≥ 60 mg/mL (Need warming) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Epigenetic Reader Domain Products |
|---|
| RVX-208
Apabetalone (RVX-208) is a first-in-class, small molecule inhibitor of BET bromodomain with IC50 of 0.51 μM for BD2. |
| I-BET151
I-BET151 (GSK1210151A) is an inhibitor of the BET family with IC50 of 0.5 μM, 0.25 μM and 0.79 μM for BRD2, BRD3 and BRD4, respectively. |
| (+)-JQ1
(+)-JQ1 is a BET bromodomain inhibitor that acts on BRD4(2) with an IC50 of 33 nM and binds to all bromodomain domains in the BET family, but not to bromodomain domains outside the BET family. JQ1 down-regulates CD47 expression through a C-MYC-mediated pathway, and JQ1 down-regulates CD47 expression through a C-MYC-mediated pathway. |
| I-BET-762
I-BET-762 (GSK525762) is a selective small molecule BET inhibitor. |
| CPI-0610
CPI-0610 is a novel BET protein bromodomain inhibitor. |
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