Cat. No.: HY-12858

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Empesertib

(Synonyms: BAY 1161909)

5 Cited Publications

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Based on 5 publication(s) in Google Scholar

Empesertib (BAY 1161909) is a potent Mps1 inhibitor, with an IC₅₀ of < 1 nM.

For research use only. We do not sell to patients.

Purity: 99.22%
CAS No.: 1443763-60-7
Formula: C₂₉H₂₆FN₅O₄S
Molecular Weight:559.61

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Empesertib Chemical Structure

CAS No.: 1443763-60-7

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Clinical Trial
Chemical Information
Publications (5)
Solvent & Solubility
- In Vitro
- In Vivo
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Purity & Documentation
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Biological Activity

Description

Empesertib (BAY 1161909) is a potent Mps1 inhibitor, with an IC₅₀ of < 1 nM.

IC₅₀ & Target^[1]

Mps1

1 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	6.9 x 10^-8mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human A2780 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human A2780 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
A2780cis	IC₅₀	6 x 10^-8mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human A2780cis cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human A2780cis cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
A-375	IC₅₀	1 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human A-375 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human A-375 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
A549	IC₅₀	1.3 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
A673	IC₅₀	9.3 x 10^-8mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human A673 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human A673 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
Caco-2	IC₅₀	1.8 x 10^-6mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human Caco-2 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human Caco-2 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
CAL-33	IC₅₀	1.1 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human CAL-33 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human CAL-33 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
Calu-6	IC₅₀	>3 x 10^-6mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human Calu-6 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human Calu-6 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
COLO 320DM	IC₅₀	1.1 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human COLO 320DM cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human COLO 320DM cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
COLO-829	IC₅₀	3 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human COLO-829 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human COLO-829 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
DU-145	IC₅₀	1.6 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
FaDu	IC₅₀	2.7 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human FaDu cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human FaDu cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
Granta-519	IC₅₀	2.4 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human Granta-519 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human Granta-519 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
HBL1	IC₅₀	1.1 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human HBL1 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human HBL1 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
HCC70	IC₅₀	8.7 x 10^-8mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human HCC70 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human HCC70 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
HCT-116	IC₅₀	4.2 x 10^-8mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human TP53 wildtype HCT-116 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human TP53 wildtype HCT-116 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
HCT-116	IC₅₀	5.6 x 10^-8mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
HCT-116	IC₅₀	5.9 x 10^-8mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human TP53 mutant HCT-116 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human TP53 mutant HCT-116 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
HCT-15	IC₅₀	1.1 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human HCT-15 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human HCT-15 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
HeLa	IC₅₀	2.6 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human HeLa cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human HeLa cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
HeLa	IC₅₀	260 nM Compound: 41; BAY 1161909	Antiproliferative activity against human HeLa cells after 96 hrs by crystal violet staining based assay Antiproliferative activity against human HeLa cells after 96 hrs by crystal violet staining based assay	[PMID: 32338514]
HeLa	IC₅₀	53 nM Compound: 41; BAY 1161909	Inhibition of MPS1 in human HeLa cells assessed as reduction in spindle assembly checkpoint incubated for 4 hrs by p-histone H3/Hoechst 33342 staining based microscopic analysis Inhibition of MPS1 in human HeLa cells assessed as reduction in spindle assembly checkpoint incubated for 4 hrs by p-histone H3/Hoechst 33342 staining based microscopic analysis	[PMID: 32338514]
HeLa	IC₅₀	56 nM Compound: Chemical Probe: BAY 1161909	Induction of cell cycle arrest in human HeLa cells assessed as metaphase arrest at 0.005 to 10 uM incubated for 4 hrs in the presence of nocodazole Induction of cell cycle arrest in human HeLa cells assessed as metaphase arrest at 0.005 to 10 uM incubated for 4 hrs in the presence of nocodazole	[PMID: 26832791]
HT-1080	IC₅₀	4.5 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human HT-1080 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human HT-1080 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
HT1197	IC₅₀	>3 x 10^-6mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human HT1197 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human HT1197 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
HT-1376	IC₅₀	3 x 10^-6mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human HT-1376 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human HT-1376 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
HT-29	IC₅₀	1 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
IGROV-1	IC₅₀	2.4 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human IGROV-1 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human IGROV-1 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
JeKo-1	IC₅₀	6.5 x 10^-8mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human JeKo-1 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human JeKo-1 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
JJN-3	IC₅₀	1 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human JJN-3 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human JJN-3 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
KM-H2	IC₅₀	2.2 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human KM-H2 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human KM-H2 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
KU-19-19	IC₅₀	8.6 x 10^-8mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human KU-19-19 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human KU-19-19 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
L-363	IC₅₀	3.2 x 10^-8mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human L-363 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human L-363 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
LAPC4	IC₅₀	1.3 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human LAPC4 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human LAPC4 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
LoVo	IC₅₀	9.5 x 10^-8mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human LoVo cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human LoVo cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
LS174T	IC₅₀	3.4 x 10^-6mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human LS174T cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human LS174T cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
Malme-3M	IC₅₀	2 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human Malme-3M cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human Malme-3M cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
MDA-MB-231	IC₅₀	1.1 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
MDA-MB-453	IC₅₀	>3 x 10^-6mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human MDA-MB-453 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human MDA-MB-453 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
MDA-MB-468	IC₅₀	3.4 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
MIA PaCa-2	IC₅₀	1 x 10^-6mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human MIA PaCa-2 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human MIA PaCa-2 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
MSTO-211H	IC₅₀	7 x 10^-8mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human MSTO-211H cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human MSTO-211H cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
NCI-H1155	IC₅₀	1.4 x 10^-6mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human NCI-H1155 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human NCI-H1155 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
NCI-H1299	IC₅₀	1.2 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human NCI-H1299 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human NCI-H1299 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
NCI-H1373	IC₅₀	1.9 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human NCI-H1373 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human NCI-H1373 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
NCI-H1650	IC₅₀	1.3 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human NCI-H1650 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human NCI-H1650 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
NCI-H1770	IC₅₀	1 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human NCI-H1770 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human NCI-H1770 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
NCI-H2009	IC₅₀	5.6 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human NCI-H2009 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human NCI-H2009 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
NCI-H2030	IC₅₀	7 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human NCI-H2030 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human NCI-H2030 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
NCI-H2052	IC₅₀	9.6 x 10^-8mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human NCI-H2052 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human NCI-H2052 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
NCI-H2228	IC₅₀	>3 x 10^-6mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human NCI-H2228 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human NCI-H2228 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
NCI-H23	IC₅₀	9.1 x 10^-8mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human NCI-H23 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human NCI-H23 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
NCI-H2452	IC₅₀	1.2 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human NCI-H2452 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human NCI-H2452 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
NCI-H28	IC₅₀	1.1 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human NCI-H28 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human NCI-H28 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
NCI-H292	IC₅₀	1.9 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human NCI-H292 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human NCI-H292 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
NCI-H460	IC₅₀	1.1 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human NCI-H460 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human NCI-H460 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
NCI-H526	IC₅₀	1 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human NCI-H526 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human NCI-H526 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
NCI-H647	IC₅₀	5.7 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human NCI-H647 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human NCI-H647 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
NCI-H661	IC₅₀	2.6 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human NCI-H661 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human NCI-H661 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
OCI-LY19	IC₅₀	6.1 x 10^-8mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human OCILY19 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human OCILY19 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
OPM-2	IC₅₀	1.3 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human OPM-2 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human OPM-2 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
OV-90	IC₅₀	1.5 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human OV-90 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human OV-90 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
OVCAR-8	IC₅₀	1.9 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human OVCAR-8 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human OVCAR-8 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
RD	IC₅₀	2.6 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human RD cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human RD cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
RKO	IC₅₀	3.9 x 10^-8mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human TP53 wildtype RKO cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human TP53 wildtype RKO cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
RKO	IC₅₀	4.8 x 10^-8mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human TP53 mutant RKO cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human TP53 mutant RKO cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
RPMI-2650	IC₅₀	5.1 x 10^-8mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human RPMI-2650 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human RPMI-2650 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
RPMI-7951	IC₅₀	2.8 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human RPMI-7951 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human RPMI-7951 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
RT-112	IC₅₀	8.3 x 10^-8mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human RT-112 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human RT-112 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
SAOS-2	IC₅₀	5.2 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human SAOS-2 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human SAOS-2 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
SiHa	IC₅₀	6.1 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human SiHa cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human SiHa cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
SJRH30	IC₅₀	4.5 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human Rh30 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human Rh30 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
SK-BR-3	IC₅₀	>3 x 10^-6mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human SK-BR-3 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human SK-BR-3 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
SK-MEL-28	IC₅₀	6.7 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
SK-MEL3	IC₅₀	5.3 x 10^-8mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human SK-MEL3 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human SK-MEL3 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
SK-MES-1	IC₅₀	2.1 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human SK-MES-1 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human SK-MES-1 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
SK-N-AS	IC₅₀	9.7 x 10^-8mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human SK-N-AS cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human SK-N-AS cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
SK-OV-3	IC₅₀	3.7 x 10^-6mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
SNU-16	IC₅₀	8.8 x 10^-8mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human SNU-16 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human SNU-16 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
TMD8	IC₅₀	2.4 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human TMD8 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human TMD8 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
U2OS	IC₅₀	5.5 x 10^-7mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human U2OS cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human U2OS cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
VCaP	IC₅₀	>3 x 10^-6mol/L Compound: Chemical Probe: BAY 1161909	Antiproliferative activity against human VCaP cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human VCaP cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]

In Vitro

BAY 1161909 is a potent Mps1 inhibitor, with an IC₅₀ of < 1 nM. BAY 1161909 also shows anti-tumor effect, suppressing the proliferation of Hela cells, with an IC₅₀ of < 400 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1443763-60-7
Appearance Solid
Molecular Weight 559.61
Formula C₂₉H₂₆FN₅O₄S
Color White to pink
SMILES

FC1=CC=C([C@@H](C)C(NC2=CC=C(C3=CN4N=C(NC5=CC=C(S(C)(=O)=O)C=C5OC)N=C4C=C3)C=C2)=O)C=C1
Synonyms

BAY 1161909
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (5)

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Cell Rep

High-Complexity shRNA Libraries and PI3 Kinase Inhibition in Cancer: High-Fidelity Synthetic Lethality Predictions. [Abstract]

2019 Apr 9;27(2):631-647.e5. PMID: 30970263
Neoplasia

Targeting monopolar spindle kinase I (Mps1 or TTK) induces radiosensitization in syngeneic models of triple negative breast cancer (TNBC) and potentiates type I interferon (T1IFN) signaling. [Abstract]

2025 Jun 10:66:101190. PMID: 40499340
Oncol Rep

Energy‑stress‑mediated activation of AMPK sensitizes MPS1 kinase inhibition in triple‑negative breast cancer. [Abstract]

2024 Aug;52(2):101. PMID: 38904203
University of Michigan

2025.
University of Gothenburg

2023 Jun 27.

Solvent & Solubility

In Vitro:

DMSO : ≥ 35 mg/mL (62.54 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7870 mL

8.9348 mL

17.8696 mL

5 mM

0.3574 mL

1.7870 mL

3.5739 mL

10 mM

0.1787 mL

0.8935 mL

1.7870 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.47 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (4.47 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.47 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Kinase Assay^[1]

N-terminally GST-tagged human full length recombinant Mps-1 kinase is used. As substrate for the kinase reaction a biotinylated peptide of the amino-acid sequence PWDPDDADITEILG is used. For the assay 50 nL of a 100-fold concentrated solution of the test compounds (BAY 1161909, etc.) in DMSO is pipetted into a black low volume 384 well microtiter plate, 2 μL of a solution of Mps-1 in assay buffer [0.1 mM sodium-ortho-vanadate, 10 mM MgCl₂, 2 mM DTT, 25 mM Hepes pH 7.7, 0.05% BSA, 0.001 % Pluronic F-127] are added and the mixture is incubated for 15 min at 22°C to allow pre-binding of the test compounds to Mps-1 before the start of the kinase reaction. Then the kinase reaction is started by the addition of 3 μL of a solution of 16.7 adenosine-tri-phosphate and peptide substrate in assay buffer and the resulting mixture is incubated for a reaction time of 60 min at 22°C. The concentration of Mps-1 in the assay is adjusted to the activity of the enzyme lot and is chosen appropriate to have the assay in the linear range, typical enzyme concentrations are in the range of about 1 nM (final cone, in the 5 μL assay volume). The reaction is stopped by the addition of 3 μL of a solution of HTRF detection reagents (100 mM Hepes pH 7.4, 0.1 % BSA, 40 mM EDTA, 140 nM Streptavidin-XLent, 1 .5 nM anti-phospho(Ser/Thr)-Europium-antibody^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[1]

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 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. The IC₅₀ values are determined by means of a 4 parameter fit. The compounds A1 (BAY 1161909), A2, A3, A4 and A5 are characterized by an IC₅₀ determined in a HeLa-MaTu-ADR cell proliferation assay^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

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

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7870 mL	8.9348 mL	17.8696 mL	44.6740 mL
	5 mM	0.3574 mL	1.7870 mL	3.5739 mL	8.9348 mL
	10 mM	0.1787 mL	0.8935 mL	1.7870 mL	4.4674 mL
	15 mM	0.1191 mL	0.5957 mL	1.1913 mL	2.9783 mL
	20 mM	0.0893 mL	0.4467 mL	0.8935 mL	2.2337 mL
	25 mM	0.0715 mL	0.3574 mL	0.7148 mL	1.7870 mL
	30 mM	0.0596 mL	0.2978 mL	0.5957 mL	1.4891 mL
	40 mM	0.0447 mL	0.2234 mL	0.4467 mL	1.1168 mL
	50 mM	0.0357 mL	0.1787 mL	0.3574 mL	0.8935 mL
	60 mM	0.0298 mL	0.1489 mL	0.2978 mL	0.7446 mL

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Complete Stock Solution Preparation Table

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Complete Stock Solution Preparation Table

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