Home Epigenetics Epigenetic Reader Domain inhibitor BRD4 Inhibitor-10 For research use only.

BRD4 Inhibitor-10

BRD4 Inhibitor-10 is a potent BRD4-BD1 inhibitor with an IC50 of 8 nM.

BRD4 Inhibitor-10 Chemical Structure

BRD4 Inhibitor-10 Chemical Structure

CAS: 1660117-38-3

Purity & Quality Control

Batch: S857401 DMSO] 86 mg/mL] false] Ethanol] 86 mg/mL] false] Water] Insoluble] false Purity: 99.79%
99.79

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Biological Activity

Description BRD4 Inhibitor-10 is a potent BRD4-BD1 inhibitor with an IC50 of 8 nM.
Targets
BET [1] BRD4-BD1 [1]
(Cell-free assay)		 BRD4-BD2 [1]
(Cell-free assay)
5 nM 41 nM
In vitro
In vitro

BI 894999 is highly active in AML cell lines, primary patient samples. BI 894999 targets super-enhancer-regulated oncogenes and other lineage-specific factors, which are involved in the maintenance of the disease state. [1]
Cell Research Cell lines MV-4-11B, THP-1, MOLM-13
Concentrations 10 nM, 100 nM, various concentrations
Incubation Time 4h, 24h, 79 h, 96 h
Method

For viability assay, the cells are plated in 96-well flat-bottom microtiter plates and incubated overnight at 37°C in a CO2 incubator. BI 894999 is added at various concentrations for 72 hours or 96 hours. After 6-hour incubation with Alamar Blue solution at 37°C, fluorescence is measured using an excitation wavelength of 531 nm and emission at 595 nm.
In Vivo
In vivo

BI 894999 is active as monotherapy in AML xenografts, and in addition leads to strongly enhanced antitumor effects in combination with CDK9 inhibitors. [1]
Animal Research Animal Models 6-8 week old female NMRI-nude/CIEA-NOG mice
Dosages 1 mg/kg, 2 mg/kg, 4 mg/kg, 12 mg/kg
Administration Oral gavage

Chemical Information & Solubility

Molecular Weight 429.51 Formula

C25H27N5O2
CAS No. 1660117-38-3 SDF --
Smiles CC1=CC(=NN(C1=O)C)C2=NC3=CN=C(C=C3N2C(C)C4=CC=CC=C4)C5CCOCC5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 86 mg/mL ( (200.22 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 86 mg/mL

Water : 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. )

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.

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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