BRD4 Inhibitor-10

Catalog No.S8574 Batch:S857401

Technical Data

Formula	C₂₅H₂₇N₅O₂
Molecular Weight	429.51	CAS No.	1660117-38-3
Solubility (25°C)*	In vitro	DMSO	86 mg/mL (200.22 mM)
		Ethanol	86 mg/mL (200.22 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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 (from reference)

Cell Assay:^{^[1]}	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.
Animal Study:^{^[1]}	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

Cell Assay:^{^[1]}

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.

Animal Study:^{^[1]}

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

References

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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