BI 894999

For research use only.

Catalog No.S8574

BI 894999 Chemical Structure

CAS No. 1660117-38-3

BI 894999 is a potent and selective BET inhibitor with IC50 of 5 nM and 41 nM for the binding of BRD4-BD1 and BRD4-BD2 to acetylated histones, respectively. BI 894999 is highly selective for BRD2/3/4 and BRDT (Kd of 0.49-1.6 nM), with at least a 200-fold selectivity vs. BRD4-BD1.

Purity & Quality Control

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Biological Activity

Description BI 894999 is a potent and selective BET inhibitor with IC50 of 5 nM and 41 nM for the binding of BRD4-BD1 and BRD4-BD2 to acetylated histones, respectively. BI 894999 is highly selective for BRD2/3/4 and BRDT (Kd of 0.49-1.6 nM), with at least a 200-fold selectivity vs. BRD4-BD1.
Targets
BET [1]
()
BRD4-BD1 [1]
(Cell-free assay)
BRD4-BD2 [1]
(Cell-free assay)
5 nM 41 nM
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]

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]

Protocol

Cell Research:

[1]

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  • 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.


    (Only for Reference)
Animal Research:

[1]

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  • 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
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 86 mg/mL (200.22 mM)
Ethanol 86 mg/mL (200.22 mM)
Water 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.

Chemical Information

Molecular Weight 429.51
Formula

C25H27N5O2

CAS No. 1660117-38-3
Storage powder
in solvent
Synonyms N/A
Smiles CC1=CC(=NN(C1=O)C)C2=NC3=CN=C(C=C3N2C(C)C4=CC=CC=C4)C5CCOCC5

In vivo Formulation Calculator (Clear solution)

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

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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

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

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Epigenetic Reader Domain Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID