PLX51107

Catalog No.S8739 Batch:S873901

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Technical Data

Formula

C26H22N4O3
Molecular Weight 438.48 CAS No. 1627929-55-8
Solubility (25°C)* In vitro DMSO 88 mg/mL (200.69 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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)		 View More
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 (from reference)

Animal Study:

[1]
  • 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

Selleck's PLX51107 has been cited by 6 publications

Inhibition of BET Proteins Regulates Fcγ Receptor Function and Reduces Inflammation in Rheumatoid Arthritis [ Int J Mol Sci, 2023, 24(8)7623] PubMed: 37108786
Inhibition of BET Family Proteins Suppresses African Swine Fever Virus Infection [ Microbiol Spectr, 2022, 10(4):e0241921] PubMed: 35758684
Epigenetic Treatment of Urothelial Carcinoma Cells Sensitizes to Cisplatin Chemotherapy and PARP Inhibitor Treatment [ Cancers (Basel), 2021, 13(6)1376] PubMed: 33803654
BRD4 Prevents R-Loop Formation and Transcription-Replication Conflicts by Ensuring Efficient Transcription Elongation [ Cell Rep, 2020, 32(12):108166] PubMed: 32966794
BRDT is a novel regulator of eIF4EBP1 in renal cell carcinoma [ Oncol Rep, 2020, 44(6):2475-2486] PubMed: 33125143
Predicting response to BET inhibitors using computational modeling: A BEAT AML project study. [ Leuk Res, 2019, 77:42-50] PubMed: 30642575

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.