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PLX51107

Cat. No. M9100
PLX51107 Structure
Synonym:

PLX-51107

Size Price Availability Quantity
10mM*1mL USD 205  USD205 In stock
5mg USD 187  USD187 In stock
10mg USD 325  USD325 In stock
25mg USD 650  USD650 In stock
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Quality Control & Documentation
Biological Activity

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.

Protocol (for reference only)
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
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
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Ozer HG, et al. Cancer Discov. BRD4 Profiling Identifies Critical Chronic Lymphocytic Leukemia Oncogenic Circuits and Reveals Sensitivity to PLX51107, a Novel Structurally Distinct BET Inhibitor.

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  Catalog
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Keywords: PLX51107, PLX-51107 supplier, Epigenetic Reader Domain, inhibitors, activators


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