research use only

PLX51107 BET inhibitor

Name: PLX51107
Brand: Selleck Chemicals
SKU: S8739
Availability: InStock
Rating: 5 (7 reviews)

Cat.No.S8739

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, this compound shows significant interactions only with the bromodomains of CBP and EP300 (p300) (Kd in the 100 nM range).

Chemical Structure

Molecular Weight: 438.48

Jump to

Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.88

Related Targets	HDAC JAK Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK Histone Acetyltransferase
Other BET Inhibitors	Molibresib (I-BET-762) Mivebresib (ABBV-075) Pelabresib (CPI-0610) INCB054329 Birabresib (OTX015) I-BET151 (GSK1210151A) Apabetalone (RVX-208) CPI-203 AZD5153 6-hydroxy-2-naphthoic acid PFI-1 (PF-6405761)

Solubility

In vitro
Batch:

DMSO : 88 mg/mL (200.69 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.400mg/ml (10.03mM)	Taking the 1 mL working solution as an example, add 50 μL of 88 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.550mg/ml (1.25mM)	Taking the 1 mL working solution as an example, add 50 μL of 11 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	438.48	Formula	C₂₆H₂₂N₄O₃	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1627929-55-8	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			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

Mechanism of Action

Targets/IC₅₀/Ki	BRD2 BD1 (Cell-free assay) 1.6 nM(Kd) BRD4 BD1 (Cell-free assay) 1.7 nM(Kd) BRD3 BD1 (Cell-free assay) 2.1 nM(Kd) BRDT BD1 (Cell-free assay) 5 nM(Kd) BRD2 BD2 (Cell-free assay) 5.9 nM(Kd) BRD4 BD2 (Cell-free assay) 6.1 nM(Kd) BRD3 BD2 (Cell-free assay) 6.2 nM(Kd) BRDT BD2 (Cell-free assay) 120 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). This compound induces accumulation of p21 and IκBα, reduced levels of cMYC, and modulation of pro- and anti-apoptotic proteins.
In vivo	PLX51107 is well tolerated in mice. The half-life of this compound is relative short in rodents and dogs (<3 h). It demonstrates in vivo antitumor effects in preclinical models of CLL and aggressive lymphoma.
References	[1] https://pubmed.ncbi.nlm.nih.gov/29386193/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

Tech Support

Handling Instructions

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

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):