Empesertib (BAY1161909)

Catalog No.S8214 Batch:S821402

Technical Data

Formula	C₂₉H₂₆FN₅O₄S
Molecular Weight	559.61	CAS No.	1443763-60-7
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (178.69 mM)
		Water	Insoluble
		Ethanol	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.)

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Biological Activity

Description

Empesertib (BAY1161909, Mps1-IN-5), a derivative of triazolopyridine, is an orally bioavailable, selective inhibitor of the serine/threonine monopolar spindle 1 (Mps1) kinase with IC50 of <1 nM. Empesertib has potential antineoplastic activity.

Targets

Mps1 ^[1]
(Cell-free assay)

1 nM

In vitro

Empesertib (BAY1161909) is a very effective Mps-1 inhibitor with an IC50 lower than or equal to 1 nM (more potent than 1 nM) in an Mps-1 kinase assay with a concentration of 1 μM/2 mM ATP, and an IC50 lower than 400 nM in a HeLa cell proliferation assay.^[1]

In vivo

Empesertib (BAY1161909) is a very effective Mps-1 inhibitor with a maximum oral bioavailability (Fmax) in rat that is higher than 70%, determined by means of rat liver microsomes, and a maximum oral bioavailability (Fmax) in dog that is higher than 50%, determined by means of dog liver microsomes, and a maximum oral bioavailability (Fmax) in human that is higher than 60%, determined by means of human liver microsomes.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines Cultivated tumor cells Concentrations 0.01 μM-30 μM Incubation Time 4 days Method Cultivated tumor cells are plated at a density of 5000 cells/well (MCF7, DU145, HeLa-MaTu-ADR), 3000 cells/well (NCI-H460, HeLa-MaTu, HeLa), or 1000 cells/well (B16F10) in a 96-well multititer plate in 200 μl of their 5 respective growth medium supplemented 10% fetal calf serum. After 24 hours, the cells of one plate (zero-point plate) are stained with crystal violet, while the medium of the other plates was replaced by fresh culture medium (200 μl), to which the test substances are added in various concentrations (0 μM, as well as in the range of 0.01-30 μM; The cells are incubated for 4 days in the presence of test substances. Cell proliferation is determined by staining the cells with crystal violet: the cells are fixed by adding 20 μl/measuring point of an 11 % glutaric aldehyde solution for 15 minutes at room temperature. After three washing cycles of the fixed cells 15 with water, the plates are dried at room temperature. The cells are stained by adding 100 μl/measuring point of a 0.1 % crystal violet solution (pH 3.0). After three washing cycles of the stained cells with water, the plates are dried at room temperature. The dye is dissolved by adding 100 μl/measuring point of a 10% acetic acid solution.
Animal Study:^{^[1]}	Animal Models rat, dog and humans Dosages 1-2 mg/mL Administration Oral gavage, IV

Cell Assay:^{^[1]}

Cell lines
Cultivated tumor cells
Concentrations
0.01 μM-30 μM
Incubation Time
4 days
Method
Cultivated tumor cells are plated at a density of 5000 cells/well (MCF7, DU145, HeLa-MaTu-ADR), 3000 cells/well (NCI-H460, HeLa-MaTu, HeLa), or 1000 cells/well (B16F10) in a 96-well multititer plate in 200 μl of their 5 respective growth medium supplemented 10% fetal calf serum. After 24 hours, the cells of one plate (zero-point plate) are stained with crystal violet, while the medium of the other plates was replaced by fresh culture medium (200 μl), to which the test substances are added in various concentrations (0 μM, as well as in the range of 0.01-30 μM; The cells are incubated for 4 days in the presence of test substances. Cell proliferation is determined by staining the cells with crystal violet: the cells are fixed by adding 20 μl/measuring point of an 11 % glutaric aldehyde solution for 15 minutes at room temperature. After three washing cycles of the fixed cells 15 with water, the plates are dried at room temperature. The cells are stained by adding 100 μl/measuring point of a 0.1 % crystal violet solution (pH 3.0). After three washing cycles of the stained cells with water, the plates are dried at room temperature. The dye is dissolved by adding 100 μl/measuring point of a 10% acetic acid solution.

Animal Study:^{^[1]}

Animal Models
rat, dog and humans
Dosages
1-2 mg/mL
Administration
Oral gavage, IV

References

[1] Volker Schulze, et al. WO2014198647A2.

Selleck's Empesertib (BAY1161909) has been cited by 1 publication

The HIPK2/CDC14B-MeCP2 axis enhances the spindle assembly checkpoint block by promoting cyclin B translation [ Sci Adv, 2023, 9(3):eadd6982]	PubMed: 36662865

The HIPK2/CDC14B-MeCP2 axis enhances the spindle assembly checkpoint block by promoting cyclin B translation [ Sci Adv, 2023, 9(3):eadd6982]

PubMed: 36662865

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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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