PLX51107

Catalog No.S8739

PLX51107 Chemical Structure

Molecular Weight(MW): 438.48

PLX51107 is as a novel BET inhibitor with modest preference for bromodomain-1 (BD1) versus bromodomain-2 (BD2) within each BET protein (Kd = 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. Among non-BET proteins, PLX51107 shows significant interactions only with the bromodomains of CBP and EP300 (p300) (Kd in the 100 nM range).

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Biological Activity

Description PLX51107 is as a novel BET inhibitor with modest preference for bromodomain-1 (BD1) versus bromodomain-2 (BD2) within each BET protein (Kd = 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. Among non-BET proteins, PLX51107 shows significant interactions only with the bromodomains of CBP and EP300 (p300) (Kd in the 100 nM range).
Targets
BRD2 BD1 [1]
(Cell-free assay)
BRD4 BD1 [1]
(Cell-free assay)
BRD3 BD1 [1]
(Cell-free assay)
BRDT BD1 [1]
(Cell-free assay)
BRD2 BD2 [1]
(Cell-free assay)
1.6 nM(Kd) 1.7 nM(Kd) 2.1 nM(Kd) 5 nM(Kd) 5.9 nM(Kd)
In vitro

In a set of cell cultures, short-term (4h) treatment of PLX51107 result in robust change in PD markers but do not induce an immediate apoptotic response. Induction of apoptosis occurrs after prolonged treatment (16 hours or more of continuous exposure). PLX51107 induces accumulation of p21 and IκBα, reduced levels of cMYC, and modulation of pro- and anti-apoptotic proteins[1].

In vivo

PLX51107 is well tolerated in mice. The half-life of PLX51107 is relative short in rodents and dogs (<3 h). PLX51107 demonstrates in vivo antitumor effects in preclinical models of CLL and aggressive lymphoma[1].

Protocol

Animal Research:

[1]

- Collapse
  • Animal Models: CD-1 mice, Sprague-Dawley rats, Beagle dogs
  • Formulation: PLX51107 DMSO solution mixed with a vehicle consisted of 10% (w/w) solutol, 10% (w/w) ethanol and 80% (w/w) water
  • Dosages: 1 mg/kg (for mice and rats); 0.5 mg/kg (for dogs)
  • Administration: IV
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 88 mg/mL (200.69 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 438.48
Formula

C26H22N4O3

CAS No. 1627929-55-8
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Epigenetic Reader Domain Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID