BAY1217389

Name: BAY1217389
Brand: MedChemExpress
SKU: HY-12859
Rating: 5.0 (8 reviews)

Cat. No.: HY-12859 Purity: 99.91%: Data Sheet
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BAY 1217389 is a potent, and selective inhibitor of the monopolar spindle 1 (MPS1) kinase with an IC₅₀ value less than 10 nM.

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

CAS No. : 1554458-53-5

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 8 publication(s) in Google Scholar

8 Publications Citing Use of MCE BAY1217389

Cell Proliferation/Viability Assay

Flow Cytometry

Histological Imaging/Staining

: BAY1217389 purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2023 Jul 13;22(1):110. [Abstract]; Dose-response plots to BAY1217389 (10^-4-10 μM) of PC9 cells.

: BAY1217389 purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2023 Jul 13;22(1):110. [Abstract]; Cell cycle analysis of PC9-ER, PC9-GR3, PC9-GR4 and PC-GR4AZD1 clones treated with BAY1217389 (50 nM; 12-72 h).

: BAY1217389 purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2023 Jul 13;22(1):110. [Abstract]; Percentage of apoptotic/necrotic cells in NCI-H1819, MDA-MB-468, SK-MES-1 and WM793 cultures treated with BAY1217389 (50 nM; 2-8 d).

: BAY1217389 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Oct 13;13(10):868. [Abstract]; BAY1217389 (2 nM; 24 h) effectively reduced the number of C4-2B CRPC cells.

: BAY1217389 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Oct 13;13(10):868. [Abstract]; BAY1217389 (32 nM; 4-16 h) obliterated the C4-2B prostaspheres formation.

: BAY1217389 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Oct 13;13(10):868. [Abstract]; BAY1217389 (32 nM; 4 h) changed morphology and reduced size of C4-2B prostaspheres.

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Description

BAY 1217389 is a potent, and selective inhibitor of the monopolar spindle 1 (MPS1) kinase with an IC₅₀ value less than 10 nM.

IC₅₀ & Target^[1]

Mps1

0.63 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	< 3 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	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	< 3 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	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]
A549	IC₅₀	6.2 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	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]
AU565	IC₅₀	2.5 x 10^-8 mol/L Compound: Chemical Probe: BAY 1217389	Antiproliferative activity against human AU565 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human AU565 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
BT-20	IC₅₀	4.8 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	Antiproliferative activity against human BT-20 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human BT-20 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
BXPC-3	IC₅₀	< 3 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	Antiproliferative activity against human BXPC-3 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human BXPC-3 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
CAL-33	IC₅₀	< 3 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	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]
COLO 205	IC₅₀	5.8 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	Antiproliferative activity against human COLO 205 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human COLO 205 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
Caco-2	IC₅₀	9.7 x 10^-8 mol/L Compound: Chemical Probe: BAY 1217389	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]
Caov-4	IC₅₀	6.8 x 10^-8 mol/L Compound: Chemical Probe: BAY 1217389	Antiproliferative activity against human Caov-4 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human Caov-4 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
DU-145	IC₅₀	6.6 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	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]
ES-2	IC₅₀	4 x 10^-8 mol/L Compound: Chemical Probe: BAY 1217389	Antiproliferative activity against human ES2 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human ES2 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
Granta-519	IC₅₀	6.7 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	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]
HCT-116	IC₅₀	< 3 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	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-116	IC₅₀	< 3 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	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]
HT-29	IC₅₀	62 nM Compound: 79; BAY 1217389	Antiproliferative activity against human HT-29 cells after 96 hrs by crystal violet staining based assay Antiproliferative activity against human HT-29 cells after 96 hrs by crystal violet staining based assay	[PMID: 32338514]
HeLa	IC₅₀	0.11 nM Compound: Chemical Probe: BAY 1217389	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]
HeLa	IC₅₀	0.25 nM Compound: 79; BAY 1217389	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	7.6 nM Compound: 79; BAY 1217389	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	7.6 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	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]
IGROV-1	IC₅₀	1.1 x 10^-8 mol/L Compound: Chemical Probe: BAY 1217389	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]
JJN-3	IC₅₀	3.4 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	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]
JeKo-1	IC₅₀	3.5 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	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]
KG-1	IC₅₀	> 3 x 10^-7 mol/L Compound: Chemical Probe: BAY 1217389	Antiproliferative activity against human KG-1 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human KG-1 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
L-363	IC₅₀	3.4 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	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]
LoVo	IC₅₀	4.4 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	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]
MCF-10A	IC₅₀	6.7 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	Antiproliferative activity against human MCF-10A cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human MCF-10A cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
MCF7	IC₅₀	< 3 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
MDA-MB-231	IC₅₀	1.7 x 10^-8 mol/L Compound: Chemical Probe: BAY 1217389	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^-7 mol/L Compound: Chemical Probe: BAY 1217389	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	0.009 μM Compound: 3; BAY-1217389	Antiproliferative activity against human MDA-MB-468 cells assessed inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MDA-MB-468 cells assessed inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37037136]
MDA-MB-468	IC₅₀	7.7 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	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	5.7 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	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]
MOLM-13	IC₅₀	1.2 x 10^-8 mol/L Compound: Chemical Probe: BAY 1217389	Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
Maver1	IC₅₀	6.6 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	Antiproliferative activity against human MAVER-1 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human MAVER-1 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
NCI-H1155	IC₅₀	< 3 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	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	< 3 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	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-H2030	IC₅₀	2.6 x 10^-8 mol/L Compound: Chemical Probe: BAY 1217389	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-H2228	IC₅₀	> 3 x 10^-7 mol/L Compound: Chemical Probe: BAY 1217389	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-H28	IC₅₀	3.5 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	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-H460	IC₅₀	5.8 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	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]
OV-90	IC₅₀	1.4 x 10^-8 mol/L Compound: Chemical Probe: BAY 1217389	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-3	IC₅₀	> 3 x 10^-7 mol/L Compound: Chemical Probe: BAY 1217389	Antiproliferative activity against human OVCAR-3 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human OVCAR-3 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
OVCAR-4	IC₅₀	3.5 x 10^-8 mol/L Compound: Chemical Probe: BAY 1217389	Antiproliferative activity against human OVCAR-4 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human OVCAR-4 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
OVCAR-5	IC₅₀	4 x 10^-8 mol/L Compound: Chemical Probe: BAY 1217389	Antiproliferative activity against human OVCAR-5 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human OVCAR-5 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
OVCAR-8	IC₅₀	< 3 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	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]
PA-1	IC₅₀	8.8 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	Antiproliferative activity against human PA-1 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human PA-1 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
PANC-1	IC₅₀	1.5 x 10^-7 mol/L Compound: Chemical Probe: BAY 1217389	Antiproliferative activity against human PANC-1 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human PANC-1 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
PC-3	IC₅₀	3.2 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
PLC-PRF-5	IC₅₀	< 3 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	Antiproliferative activity against human PLCPRF5 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human PLCPRF5 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
RKO	IC₅₀	< 3 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	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]
RKO	IC₅₀	< 3 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	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]
RPMI-7951	IC₅₀	< 3 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	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]
Rec1	IC₅₀	7.5 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	Antiproliferative activity against human REC1 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human REC1 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
SK-BR-3	IC₅₀	< 3 x 10^-7 mol/L Compound: Chemical Probe: BAY 1217389	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	2.5 x 10^-8 mol/L Compound: Chemical Probe: BAY 1217389	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-MES-1	IC₅₀	2.6 x 10^-8 mol/L Compound: Chemical Probe: BAY 1217389	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	< 3 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	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 x 10^-7 mol/L Compound: Chemical Probe: BAY 1217389	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	4.4 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	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]
SNU1	IC₅₀	6.7 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	Antiproliferative activity against human SNU1 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human SNU1 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
TMD8	IC₅₀	6.7 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	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]
U-251	IC₅₀	9.4 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	Antiproliferative activity against human U-251 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human U-251 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
U-87MG ATCC	IC₅₀	9.7 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	Antiproliferative activity against human U-87MG cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human U-87MG cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]
Z-138	IC₅₀	6.2 x 10^-9 mol/L Compound: Chemical Probe: BAY 1217389	Antiproliferative activity against human Z138 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay Antiproliferative activity against human Z138 cells assessed as cell growth inhibition incubated for 96 hrs by MTS assay	[PMID: 26832791]

In Vitro

BAY 1217389 inhibits Mps1 kinase activity with IC₅₀ value below 10 nM while showing an excellent selectivity profile. In cellular mechanistic assays BAY 1217389 abrogates nocodazole-induced SAC activity and induces premature exit from mitosis resulting in multinuclearity and tumor cell death. BAY 1217389 efficiently inhibits tumor cell proliferation in vitro^[1].

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

In Vivo

BAY 1217389 achieves moderate efficacy in monotherapy in tumor xenograft studies. However, in line with its unique mode of action, when combines with paclitaxel, low doses of Mps1 inhibitor reduces paclitaxel-induced mitotic arrest in line with weakening of SAC activity. As a result, combination therapy strongly improves efficacy over paclitaxel or Mps1 inhibitor monotreatment at the respective MTDs in a broad range of xenograft models including those showing acquired or intrinsic paclitaxel-resistance. BAY 1217389 shows good tolerability without adding toxicity to paclitaxel monotherapy^[1].

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

Clinical Trial

Molecular Weight

561.50

Formula

C₂₇H₂₄F₅N₅O₃

CAS No.

1554458-53-5

Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1CC1)C2=CC=C(C3=CN=C4C(NCCC(F)(F)F)=CC(OC5=CC=C(OC)C(F)=C5F)=NN43)C=C2C

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

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (178.09 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7809 mL	8.9047 mL	17.8094 mL
5 mM	0.3562 mL	1.7809 mL	3.5619 mL
10 mM	0.1781 mL	0.8905 mL	1.7809 mL

View the Complete Stock Solution Preparation Table

* 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
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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 (4.45 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 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.45 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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.94%

Select Batch:

Data Sheet (282 KB) SDS (396 KB)

COA (254 KB) HNMR (222 KB) LCMS (160 KB)

Handling Instructions (2659 KB)

References

[1]. Wengner AM, et al. Novel Mps1 Kinase Inhibitors with Potent Antitumor Activity. Mol Cancer Ther. 2016 Apr;15(4):583-92.. . . . [Content Brief]

[2]. Wengner AM, et al. Novel Mps1 Kinase Inhibitors with Potent Antitumor Activity. Mol Cancer Ther. 2016 Apr;15(4):583-92.

Kinase Assay ^[1]	Inhibition of recombinant human Mps1 by BAY 1161909 or BAY 1217389 is assessed in TRFRET-based in vitro kinase assays via phosphorylation of a biotinylated peptide (Biotin-Ahx-PWDPDDADITEILG-NH2). Under standard assay conditions kinase and test compound are preincubated for 15 min before enzyme reaction is started by addition of substrate and ATP upon 10 μM^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Cells are seeded into 96 well plates at densities ranging from 1,000 to 5,000 cells per well in the appropriate medium supplemented with 10% FCS. After 24 hours, cells are treated in quadruplicates with serial dilutions of BAY 1161909 or BAY 1217389. After further 96 hours, adherent cells are fixed with glutaraldehyde and stained with crystal violet. IC₅₀ values are calculated by means of a 4 parameter fit^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice: For tumor xenograft studies female athymic NMRI nu/nu mice, 50 days old, average body weight 20-22 g, are used. When tumors reaches a size of approximately 20-40 mm², depending on growth of the tumor model, animals are randomized to treatment and control groups (8-10 mice / group) and treated p.o. with vehicle (70% polyethylene glycol 400, 5% Ethanol, 25% Solutol), BAY 1161909, BAY 1217389, and/or paclitaxel. For analysis of polyploidy and multinuclearity induction in vivo, A2780cis tumor bearing female NMRI nude mice are treated with paclitaxel (i.v. once with 24 mg/kg), BAY 1161909 p.o.twice daily for 2 days with 2.5 mg/kg and in combination with paclitaxel (i.v. once 24 mg/kg) and BAY 1161909 (p.o. twice daily for 2 days 1 mg/kg)^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Wengner AM, et al. Novel Mps1 Kinase Inhibitors with Potent Antitumor Activity. Mol Cancer Ther. 2016 Apr;15(4):583-92.. . . . [Content Brief] [2]. Wengner AM, et al. Novel Mps1 Kinase Inhibitors with Potent Antitumor Activity. Mol Cancer Ther. 2016 Apr;15(4):583-92.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7809 mL	8.9047 mL	17.8094 mL	44.5236 mL
	5 mM	0.3562 mL	1.7809 mL	3.5619 mL	8.9047 mL
	10 mM	0.1781 mL	0.8905 mL	1.7809 mL	4.4524 mL
	15 mM	0.1187 mL	0.5936 mL	1.1873 mL	2.9682 mL
	20 mM	0.0890 mL	0.4452 mL	0.8905 mL	2.2262 mL
	25 mM	0.0712 mL	0.3562 mL	0.7124 mL	1.7809 mL
	30 mM	0.0594 mL	0.2968 mL	0.5936 mL	1.4841 mL
	40 mM	0.0445 mL	0.2226 mL	0.4452 mL	1.1131 mL
	50 mM	0.0356 mL	0.1781 mL	0.3562 mL	0.8905 mL
	60 mM	0.0297 mL	0.1484 mL	0.2968 mL	0.7421 mL
	80 mM	0.0223 mL	0.1113 mL	0.2226 mL	0.5565 mL
	100 mM	0.0178 mL	0.0890 mL	0.1781 mL	0.4452 mL

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BAY12173891554458-53-5BAY 1217389BAY-1217389Mps1Monopolar spindle 1Inhibitorinhibitorinhibit

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