Home Epigenetics Epigenetic Reader Domain inhibitor PLX51107 For research use only.

PLX51107

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).

PLX51107 Chemical Structure

PLX51107 Chemical Structure

CAS No. 1627929-55-8

Purity & Quality Control

Batch: S873901 DMSO]88 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.88%
99.88

PLX51107 Related Products

Signaling Pathway

Epigenetic Reader Domain Signaling Pathways

Epigenetic Reader Domain Signaling Pathway

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)		 Click to View More Targets
1.6 nM(Kd) 1.7 nM(Kd) 2.1 nM(Kd) 5 nM(Kd) 5.9 nM(Kd)
In vitro
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
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].
Animal Research Animal Models CD-1 mice, Sprague-Dawley rats, Beagle dogs
Dosages 1 mg/kg (for mice and rats); 0.5 mg/kg (for dogs)
Administration IV
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02683395 Terminated
Solid Tumors|Acute Myeloid Leukemia|Myelodysplastic Syndrome|Non-Hodgkin''s Lymphoma
Plexxikon
 March 2016 Phase 1

Chemical Information & Solubility

Molecular Weight 438.48 Formula

C26H22N4O3
CAS No. 1627929-55-8 SDF --
Smiles CC1=C(C(=NO1)C)C2=CC3=C(C(=CN3C(C)C4=CC=CC=N4)C5=CC=C(C=C5)C(=O)O)N=C2
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 88 mg/mL ( (200.69 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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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

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