BAY1217389

目录号: HY-12859 一键复制产品信息纯度: 99.39%: Data Sheet SDS COA 产品使用指南
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BAY 1217389是具有高效性和选择性的(MPS1)激酶抑制剂，IC₅₀值小于10 nM。

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BAY1217389 Chemical Structure

CAS No. : 1554458-53-5

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1174	In-stock
2 mg	￥603	In-stock
5 mg	￥950	In-stock
10 mg	￥1425	In-stock
25 mg	￥2565	In-stock
50 mg	￥3850	In-stock
100 mg	￥5390	In-stock
200 mg		询价
500 mg		询价

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Customer Review

MCE 顾客使用本产品发表的 6 篇科研文献

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

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)

细胞效力
(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]

体外研究
(In Vitro)

BAY 1217389 抑制 Mps1 激酶活性的 IC₅₀ 值 < 10 nM，同时表现出良好的选择性。在细胞机制试验中，BAY 1217389 消除 Nocodazole 诱导的 SAC 活性，诱导有丝分裂过早退出，导致多核和肿瘤细胞死亡。BAY 1217389 体外有效抑制肿瘤细胞增殖^[1]。

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

体内研究
(In Vivo)

BAY 1217389 在异种肿瘤移植研究中单药治疗达到中等疗效。然而，根据其独特的作用方式，当紫杉醇联合使用时，低剂量 Mps1 抑制剂可以减少紫杉醇诱导的有丝分裂停止，从而减弱 SAC 活性。因此，在广泛的异种移植模型中，包括那些表现出获得性或内在紫杉醇耐药的异种移植模型中，联合治疗在各自 MTDs 上的疗效明显优于紫杉醇或 Mps1 抑制剂单药治疗。BAY 1217389 对紫杉醇单药治疗耐受性良好，不增加毒性^[1]。

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

Clinical Trial

分子量

561.50

Formula

C₂₇H₂₄F₅N₅O₃

CAS 号

1554458-53-5

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 100 mg/mL (178.09 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	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

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

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

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (4.45 mM); 悬浊液; 超声助溶

此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.45 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.94%

选择批次：

Data Sheet (648 KB) SDS (393 KB)

COA (292 KB) HNMR (222 KB) LCMS (160 KB)

产品使用指南 (1538 KB)

参考文献

[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.
参考文献	[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.

BAY1217389 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	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

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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