Empesertib

Empesertib - Names and Identifiers

Name	(2R)-2-(4-fluorophenyl)-N-[4-(2-{[2-methoxy-4-(methylsulfonyl)phenyl]-amino}[1,2,4]triazolo[1,5-a]pyridin-6-yl)phenyl]propanamide (2R)-2-(4-fluorophenyl)-N-[4-(2-{[2-methoxy-4-(methylsulfonyl)phenyl]
Synonyms	CS-2060 Mps1-IN-5 BAY1161909 Empesertib BAY-1161909 BAY 1161909 BAY-1161909 EMPESERTIB BAY-1161909 Empesertib (2R)-2-(4-fluorophenyl)-N-[4-(2-{[2-methoxy-4-(methylsulfonyl)phenyl] (2R)-2-(4-fluorophenyl)-N-[4-(2-{[2-methoxy-4-(methylsulfonyl)phenyl]-amino}[1,2,4]triazolo[1,5-a]pyridin-6-yl)phenyl]propanamide Benzeneacetamide, 4-fluoro-N-[4-[2-[[2-methoxy-4-(methylsulfonyl)phenyl]amino][1,2,4]triazolo[1,5-a]pyridin-6-yl]phenyl]-α-methyl-, (αR)-
CAS	1443763-60-7

Empesertib - Physico-chemical Properties

Molecular Formula	C29H26FN5O4S
Molar Mass	559.62
Density	1.36±0.1 g/cm3(Predicted)
Solubility	DMSO: ≥ 35 mg/mL
pKa	13.71±0.70(Predicted)
Storage Condition	-20℃
Use	Empesertib (BAY 1161909) is a potent Mps1 inhibitor, with an IC50 of < 1 nM.

Empesertib - Reference

Reference

1. SCHULZE, Volker, et al. PRODRUG DERIVATIVES OF SUBSTITUTED TRIAZOLOPYRIDINES. WO2014198647A2

Empesertib - Preparation solution concentration reference

	1mg	5mg	10mg
1 mM	1.787 ml	8.935 ml	17.87 ml
5 mM	0.357 ml	1.787 ml	3.574 ml
10 mM	0.179 ml	0.893 ml	1.787 ml
5 mM	0.036 ml	0.179 ml	0.357 ml

Last Update：2024-01-02 23:10:35

Empesertib - Cell Experiment

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 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 is replaced by fresh culture medium (200 μL), to which the test substances (BAY 1161909, etc.) are added in various concentrations (0 μM, as well as in the range of 0.01-30 μM; the final concentration of the solvent DMSO is 0.5%). 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 with water, the plates are dried at room temperature. The cells are

Last Update：2023-08-16 21:32:38