2. Epigenetics
  3. Epigenetic Reader Domain
  4. PLX51107

PLX51107 

Cat. No.: HY-111422 Purity: 99.74%
COA Handling Instructions

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 also interacts with the bromodomains of CBP and EP300 (Kd, in the 100 nM range).

For research use only. We do not sell to patients.

PLX51107 Chemical Structure

PLX51107 Chemical Structure

CAS No. : 1627929-55-8

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 165 In-stock
Solution
10 mM * 1 mL in DMSO USD 165 In-stock
Solid
5 mg USD 150 In-stock
10 mg USD 250 In-stock
50 mg USD 950 In-stock
100 mg   Get quote  
200 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 3 publication(s) in Google Scholar

PLX51107 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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 also interacts with the bromodomains of CBP and EP300 (Kd, in the 100 nM range).

IC50 & Target

Kd: 1.6 nM (BRD2-BD1), 2.1 nM (BRD3-BD1), 1.7 nM (BRD4-BD1), 5 nM (BRDT-BD1), 5.9 nM (BRD2-BD2), 6.2 nM (BRD3-BD2), 6.1 nM (BRD4-BD2), 120 nM (BRDT-BD2), ∼100 nM (CBP), ∼100 nM (EP300)[1]
In Vitro

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 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. PLX51107 selectively modulates CLL driver genes[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PLX51107 Related Antibodies
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[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

438.48

Appearance

Solid

Formula

C26H22N4O3
CAS No.
SMILES

C[C@@H](C1=NC=CC=C1)N2C=C(C3=CC=C(C(O)=O)C=C3)C4=NC=C(C5=C(C)ON=C5C)C=C42
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : 75 mg/mL (171.05 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2806 mL 11.4030 mL 22.8061 mL
5 mM 0.4561 mL 2.2806 mL 4.5612 mL
10 mM 0.2281 mL 1.1403 mL 2.2806 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.70 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.70 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.70 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.74%

COA (262 KB) LCMS (266 KB)

Handling Instructions (2659 KB)
References
Animal Administration
[1]

Mice[1]
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
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PLX51107 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

PLX511071627929-55-8PLX 51107PLX-51107Epigenetic Reader DomainInhibitorinhibitorinhibit

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