BI-9564

Catalog No.S8113 Batch:S811303

Technical Data

Formula	C₂₀H₂₃N₃O₃
Molecular Weight	353.41	CAS No.	1883429-22-8
Solubility (25°C)*	In vitro	Ethanol	7 mg/mL (19.8 mM)
		DMSO	6 mg/mL (16.97 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

BI-9564 is a selective inhibitor of BRD9 and BRD7 bromodomains with the IC50 of 75 nM and 3.4 µM, respectively.

Targets

BRD9 ^[1] (Cell-free assay)	BRD7 ^[1] (Cell-free assay)	CECR2 ^[1] (Cell-free assay)
5.9 nM(Kd)	73 nM(Kd)	77 nM(Kd)

In vitro

Treatment of the panel with BI-9564 results in selective growth inhibition of a significant proportion of AML cell lines tested^[1].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines MV-4-11 cells Concentrations various concentrations(10 nM-100 μM) Incubation Time 2 h Method To 750,000 MV-4-11 cells in 250 µl growth medium (in IMDM, 10 % FBS, GlutaMAX, 25 mM HEPES and 0,1% 2-Mercaptoethanol) per well compound is added at the desired concentration from a 10 mM stock solution using the HP D300 Digital Dispenser. After 2 hours of incubation with the compound, cells are collected by centrifugation, washed in ice cold PBS and lysed in 15 µl of cell extraction buffer. After 30 minutes on ice, nucleic acids are disrupted by sonication. cMYC levels are measured using the human c-Myc (Total) ELISA Kit.
Animal Study:^{^[1]}	Animal Models Female CIEA-NOG mice Dosages 10 mL/kg Administration Oral administration

Cell Assay:^{^[1]}

Cell lines
MV-4-11 cells
Concentrations
various concentrations(10 nM-100 μM)
Incubation Time
2 h
Method
To 750,000 MV-4-11 cells in 250 µl growth medium (in IMDM, 10 % FBS, GlutaMAX, 25 mM HEPES and 0,1% 2-Mercaptoethanol) per well compound is added at the desired concentration from a 10 mM stock solution using the HP D300 Digital Dispenser. After 2 hours of incubation with the compound, cells are collected by centrifugation, washed in ice cold PBS and lysed in 15 µl of cell extraction buffer. After 30 minutes on ice, nucleic acids are disrupted by sonication. cMYC levels are measured using the human c-Myc (Total) ELISA Kit.

Animal Study:^{^[1]}

Animal Models
Female CIEA-NOG mice
Dosages
10 mL/kg
Administration
Oral administration

References

[1] Martin LJ, et al. J Med Chem. 2016, 59(10):4462-75.

Selleck's BI-9564 has been cited by 1 publication

GSK2801, a BAZ2/BRD9 Bromodomain Inhibitor, Synergizes with BET Inhibitors to Induce Apoptosis in Triple-Negative Breast Cancer [ Mol Cancer Res, 2019, 17(7):1503-1518]	PubMed: 31000582

GSK2801, a BAZ2/BRD9 Bromodomain Inhibitor, Synergizes with BET Inhibitors to Induce Apoptosis in Triple-Negative Breast Cancer [ Mol Cancer Res, 2019, 17(7):1503-1518]

PubMed: 31000582

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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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