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PLX51107

Catalog No. TQ0253 CAS 1627929-55-8

PLX51107 is a potent and selective BET inhibitor (Kds: 1.6, 2.1, 1.7, and 5 nM for BRD2-BD1, BRD3-BD1, BRD4-BD1, and BRDT-BD1).

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PLX51107, CAS 1627929-55-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 51.00
2 mg	In stock	$ 74.00
5 mg	In stock	$ 122.00
10 mg	In stock	$ 198.00
25 mg	In stock	$ 347.00
50 mg	In stock	$ 515.00
100 mg	In stock	$ 747.00
1 mL * 10 mM (in DMSO)	In stock	$ 133.00

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Purity: 99.75%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	PLX51107 is a potent and selective BET inhibitor (Kds: 1.6, 2.1, 1.7, and 5 nM for BRD2-BD1, BRD3-BD1, BRD4-BD1, and BRDT-BD1).
Targets&IC50	BRD3 BD1:2.1 nM (Kd), BRDT BD1:5 nM (Kd), BRD4 BD2:6.1 nM (Kd), BRD4 BD1:1.7 nM (Kd), BRD3 BD2:6.2 nM (Kd), BRD2 BD2:5.9 nM (Kd), BRD2 BD1:1.6 nM (Kd), BRDT BD2:120 nM (Kd)
In vitro	PLX51107 is a 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 also interacts with the bromodomains of CBP and EP300 (Kd, in the 100 nM range). 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, q.d, p.o.) exhibits potent antileukemic effects in disease models of aggressive CLL and Richter transformation (RT) via oral administration once daily.
Animal Research	For engraftment studies, C57BL/6 WT mice are engrafted with 1E7 cells by tail-vein injection of splenocytes derived from Eμ-TCL1 or Eμ-Myc/TCL1 mice with active disease. At the onset of leukemia (Eμ-TCL1: ≥ 10% CD19/CD5/CD45-positive circulating cells; Eμ-Myc/TCL1: WBC count ≥ 8 and/or ≥ 5% CD19/CD5/CD45-positive circulating cells), mice are randomized to receive treatments as indicated. PLX51107 20 mg/kg, qd (once daily), oral gavage. Vehicle = 10% N-methyl-2-pyrrolidone plus diluent (40% PEG400, 5% TPGS, 5% Poloxamer 407, and 50% water). Mice are sacrificed when meeting early removal criteria (>20% weight loss, impaired motility, splenomegaly, and evident tumor masses), and tissues are collected for further analysis.

Molecular Weight	438.48
Formula	C26H22N4O3
CAS No.	1627929-55-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 70 mg/mL (159.65 mM), Sonication is recommended.

References and Literature

1. Ozer HG, et al. BRD4 Profiling Identifies Critical Chronic Lymphocytic Leukemia Oncogenic Circuits and Reveals Sensitivity to PLX51107, a Novel Structurally Distinct BET Inhibitor. Cancer Discov. 2018 Apr;8(4):458-477.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Reprogramming Compound Library NO PAINS Compound Library Anti-Cancer Compound Library Hematonosis Compound Library Clinical Compound Library

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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.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

PLX51107 1627929-55-8 Chromatin/Epigenetic Epigenetic Reader Domain PLX 51107 PLX-51107 inhibit Inhibitor inhibitor

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