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NMS-P715

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NMS-P715 is a selective, ATP-competitive inhibitor of MPS1, with an IC₅₀ of 182 nM.

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Reinheit: 99.30%
CAS. Nr.: 1202055-32-0
Formel: C₃₅H₃₉F₃N₈O₃
Molecular Weight:676.73

Speicherung:

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

NMS-P715 Chemical Structure

CAS. Nr.: 1202055-32-0

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Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
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Biologische Aktivität

Beschreibung

NMS-P715 is a selective, ATP-competitive inhibitor of MPS1, with an IC₅₀ of 182 nM.

IC₅₀ & Target^[1]

Mps1

182 nM (IC₅₀)

CK2

5.7 μM (IC₅₀)

MELK

6.01 μM (IC₅₀)

NEK6

6.02 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
786-0	IC₅₀	0.917 μM Compound: NMS-P715	Antiproliferative activity against human 786-0 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human 786-0 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
A2780	IC₅₀	1 μM Compound: 15, NMS-P715	Antiproliferative activity in human A2780 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity in human A2780 cells after 72 hrs by CellTiter-Glo assay	[PMID: 21723120]
A2780	IC₅₀	1 μM Compound: NMS-P715	Antiproliferative activity against human A2780 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human A2780 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
A-375	IC₅₀	0.796 μM Compound: NMS-P715	Antiproliferative activity against human A-375 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human A-375 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
A-431	IC₅₀	0.469 μM Compound: NMS-P715	Antiproliferative activity against human A-431 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human A-431 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
A498	IC₅₀	1.706 μM Compound: NMS-P715	Antiproliferative activity against human A498 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human A498 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
A549	IC₅₀	1.249 μM Compound: NMS-P715	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
A549	IC₅₀	1.25 μM Compound: 1, NMS-P715	Antiproliferative activity against human A549 cells after 72 hrs by WST8 assay Antiproliferative activity against human A549 cells after 72 hrs by WST8 assay	[PMID: 23634759]
ACHN	IC₅₀	0.015 μM Compound: NMS-P715	Antiproliferative activity against human ACHN cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human ACHN cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
BJ	IC₅₀	5.473 μM Compound: NMS-P715	Antiproliferative activity against human BJ cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human BJ cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
BT-474	IC₅₀	1.157 μM Compound: NMS-P715	Antiproliferative activity against human BT-474 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human BT-474 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
BT-549	IC₅₀	1.049 μM Compound: NMS-P715	Antiproliferative activity against human BT-549 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human BT-549 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
BXPC-3	IC₅₀	2.179 μM Compound: NMS-P715	Antiproliferative activity against human BXPC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human BXPC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
C-33-A	IC₅₀	3.012 μM Compound: NMS-P715	Antiproliferative activity against human C-33-A cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human C-33-A cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
CAKI-1	IC₅₀	1.997 μM Compound: NMS-P715	Antiproliferative activity against human CAKI-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human CAKI-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
Calu-3	IC₅₀	1.439 μM Compound: NMS-P715	Antiproliferative activity against human Calu-3 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human Calu-3 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
CAPAN-1	IC₅₀	5.224 μM Compound: NMS-P715	Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
CCRF-CEM	IC₅₀	1.432 μM Compound: NMS-P715	Antiproliferative activity against human CCRF-CEM cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human CCRF-CEM cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
COLO 205	IC₅₀	0.592 μM Compound: NMS-P715	Antiproliferative activity against human COLO 205 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human COLO 205 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
COLO 320	IC₅₀	1.284 μM Compound: NMS-P715	Antiproliferative activity against human COLO 320 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human COLO 320 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
COLO-678	IC₅₀	10 μM Compound: NMS-P715	Antiproliferative activity against human COLO-678 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human COLO-678 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
COLO-741	IC₅₀	10 μM Compound: NMS-P715	Antiproliferative activity against human COLO-741 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human COLO-741 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
DLD-1	IC₅₀	1017 nM Compound: Chemical probe: NMS-P715	Inhibition of colony formation in human DLD-1 cells harboring Mps1 S611R mutant assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay Inhibition of colony formation in human DLD-1 cells harboring Mps1 S611R mutant assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay	[PMID: 26364596]
DLD-1	IC₅₀	164.8 nM Compound: Chemical probe: NMS-P715	Antiproliferative activity against human DLD-1 cells assessed as reduction in cell viability incubated for 5 days Antiproliferative activity against human DLD-1 cells assessed as reduction in cell viability incubated for 5 days	[PMID: 26364596]
DLD-1	IC₅₀	198 nM Compound: Chemical probe: NMS-P715	Inhibition of colony formation in human DLD-1 cells assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay Inhibition of colony formation in human DLD-1 cells assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay	[PMID: 26364596]
DU-145	IC₅₀	1.932 μM Compound: NMS-P715	Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
EKVX	IC₅₀	6.976 μM Compound: NMS-P715	Antiproliferative activity against human EKVX cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human EKVX cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
Granta-519	IC₅₀	1.687 μM Compound: NMS-P715	Antiproliferative activity against human Granta-519 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human Granta-519 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
HCC 2998	IC₅₀	1.813 μM Compound: NMS-P715	Antiproliferative activity against human HCC 2998 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human HCC 2998 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
HCC78	IC₅₀	10 μM Compound: NMS-P715	Antiproliferative activity against human HCC78 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human HCC78 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
HCT-116	GI₅₀	0.18 μM Compound: 5, NMS-P715	Growth inhibition in human HCT116 cells after 72 hrs by MTT assay Growth inhibition in human HCT116 cells after 72 hrs by MTT assay	[PMID: 24256217]
HCT-116	IC₅₀	>2000 nM Compound: Chemical probe: NMS-P715	Inhibition of colony formation in human HCT-116 cells harboring Mps1 C604Y mutant assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay Inhibition of colony formation in human HCT-116 cells harboring Mps1 C604Y mutant assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay	[PMID: 26364596]
HCT-116	IC₅₀	0.16 μM Compound: 5, NMS-P715	Inhibition of Myc-tagged wild type MPS1 autophosphorylation in human HCT116 cells after 2 hrs in presence of proteosome inhibitor MG132 Inhibition of Myc-tagged wild type MPS1 autophosphorylation in human HCT116 cells after 2 hrs in presence of proteosome inhibitor MG132	[PMID: 24256217]
HCT-116	IC₅₀	153.8 nM Compound: Chemical probe: NMS-P715	Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 5 days Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 5 days	[PMID: 26364596]
HCT-116	IC₅₀	1625 nM Compound: Chemical probe: NMS-P715	Inhibition of colony formation in human HCT-116 cells harboring Mps1 I531M mutant assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay Inhibition of colony formation in human HCT-116 cells harboring Mps1 I531M mutant assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay	[PMID: 26364596]
HCT-116	IC₅₀	171 nM Compound: Chemical probe: NMS-P715	Inhibition of colony formation in human HCT-116 cells assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay Inhibition of colony formation in human HCT-116 cells assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay	[PMID: 26364596]
HCT-116	IC₅₀	2.036 μM Compound: NMS-P715	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
HCT-15	IC₅₀	0.232 μM Compound: NMS-P715	Antiproliferative activity against human HCT-15 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human HCT-15 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
HEL	IC₅₀	5.486 μM Compound: NMS-P715	Antiproliferative activity against human HEL cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human HEL cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
HeLa	IC₅₀	>2000 nM Compound: Chemical probe: NMS-P715	Inhibition of colony formation in human HeLa cells harboring Mps1 C604Y mutant assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay Inhibition of colony formation in human HeLa cells harboring Mps1 C604Y mutant assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay	[PMID: 26364596]
HeLa	IC₅₀	1330 nM Compound: Chemical probe: NMS-P715	Inhibition of colony formation in human HeLa cells harboring Mps1 I598F mutant assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay Inhibition of colony formation in human HeLa cells harboring Mps1 I598F mutant assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay	[PMID: 26364596]
HeLa	IC₅₀	1720 nM Compound: Chemical probe: NMS-P715	Inhibition of colony formation in human HeLa cells harboring Mps1 C604F mutant assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay Inhibition of colony formation in human HeLa cells harboring Mps1 C604F mutant assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay	[PMID: 26364596]
HeLa	IC₅₀	433 nM Compound: Chemical probe: NMS-P715	Inhibition of colony formation in human HeLa cells assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay Inhibition of colony formation in human HeLa cells assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay	[PMID: 26364596]
HeLa	IC₅₀	6.46 μM Compound: NMS-P715	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
HL-60	IC₅₀	1.584 μM Compound: NMS-P715	Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
HOP-62	IC₅₀	7.771 μM Compound: NMS-P715	Antiproliferative activity against human HOP-62 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human HOP-62 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
HOP-92	IC₅₀	2.178 μM Compound: NMS-P715	Antiproliferative activity against human HOP-92 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human HOP-92 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
Hs-578T	IC₅₀	6.638 μM Compound: NMS-P715	Antiproliferative activity against human Hs-578T cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human Hs-578T cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
HT1197	IC₅₀	8.304 μM Compound: NMS-P715	Antiproliferative activity against human HT1197 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human HT1197 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
HT-29	IC₅₀	3.918 μM Compound: NMS-P715	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
IGROV-1	IC₅₀	1.152 μM Compound: NMS-P715	Antiproliferative activity against human IGROV-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human IGROV-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
Jurkat	IC₅₀	3.606 μM Compound: NMS-P715	Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
K562	IC₅₀	2.705 μM Compound: NMS-P715	Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
KARPAS-299	IC₅₀	3.533 μM Compound: NMS-P715	Antiproliferative activity against human KARPAS-299 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human KARPAS-299 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
KG-1	IC₅₀	2.958 μM Compound: NMS-P715	Antiproliferative activity against human KG-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human KG-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
KM12	IC₅₀	0.586 μM Compound: NMS-P715	Antiproliferative activity against human KM12 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human KM12 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
L-363	IC₅₀	1.607 μM Compound: NMS-P715	Antiproliferative activity against human L-363 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human L-363 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
LNCaP	IC₅₀	3.072 μM Compound: NMS-P715	Antiproliferative activity against human LNCaP cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human LNCaP cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
LoVo	IC₅₀	1.87 μM Compound: NMS-P715	Antiproliferative activity against human LoVo cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human LoVo cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
LP-1	IC₅₀	3.479 μM Compound: NMS-P715	Antiproliferative activity against human LP-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human LP-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
LS174T	IC₅₀	1.936 μM Compound: NMS-P715	Antiproliferative activity against human LS174T cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human LS174T cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
LS180	IC₅₀	2.168 μM Compound: NMS-P715	Antiproliferative activity against human LS180 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human LS180 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
M14	IC₅₀	0.698 μM Compound: NMS-P715	Antiproliferative activity against human M14 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human M14 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
MCF7	IC₅₀	1.86 μM Compound: NMS-P715	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
MDA-MB-231	IC₅₀	0.899 μM Compound: NMS-P715	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
MDA-MB-435	IC₅₀	1.955 μM Compound: NMS-P715	Antiproliferative activity against human MDA-MB-435 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human MDA-MB-435 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
MeWo	IC₅₀	3.257 μM Compound: NMS-P715	Antiproliferative activity against human MeWo cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human MeWo cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
MIA PaCa-2	IC₅₀	2.549 μM Compound: NMS-P715	Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
MOLM-13	IC₅₀	1.041 μM Compound: NMS-P715	Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
MOLT-4	IC₅₀	1.041 μM Compound: NMS-P715	Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
MV4-11	IC₅₀	1.141 μM Compound: NMS-P715	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
NCI/ADR-RES	IC₅₀	2.484 μM Compound: NMS-P715	Antiproliferative activity against human NCI-ADR-RES cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-ADR-RES cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
NCI-H146	IC₅₀	4.283 μM Compound: NMS-P715	Antiproliferative activity against human NCI-H146 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-H146 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
NCI-H1770	IC₅₀	4.415 μM Compound: NMS-P715	Antiproliferative activity against human NCI-H1770 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-H1770 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
NCI-H1975	IC₅₀	10 μM Compound: NMS-P715	Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
NCI-H2126	IC₅₀	4.632 μM Compound: NMS-P715	Antiproliferative activity against human NCI-H2126 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-H2126 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
NCI-H2228	IC₅₀	5.812 μM Compound: NMS-P715	Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
NCI-H226	IC₅₀	2.007 μM Compound: NMS-P715	Antiproliferative activity against human NCI-H226 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-H226 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
NCI-H23	IC₅₀	1.216 μM Compound: NMS-P715	Antiproliferative activity against human NCI-H23 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-H23 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
NCI-H322M	IC₅₀	1.555 μM Compound: NMS-P715	Antiproliferative activity against human NCI-H322M cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-H322M cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
NCI-H460	IC₅₀	2.191 μM Compound: NMS-P715	Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
NCI-H522	IC₅₀	1.205 μM Compound: NMS-P715	Antiproliferative activity against human NCI-H522 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-H522 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
NCI-H526	IC₅₀	2.203 μM Compound: NMS-P715	Antiproliferative activity against human NCI-H526 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-H526 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
NCI-H82	IC₅₀	2.59 μM Compound: NMS-P715	Antiproliferative activity against human NCI-H82 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-H82 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
NCI-H889	IC₅₀	1.26 μM Compound: NMS-P715	Antiproliferative activity against human NCI-H889 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-H889 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
NCI-H929	IC₅₀	10 μM Compound: NMS-P715	Antiproliferative activity against human NCI-H929 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-H929 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
NHDF	IC₅₀	10 μM Compound: NMS-P715	Antiproliferative activity against human NHDF cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NHDF cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
OPM-2	IC₅₀	2.31 μM Compound: NMS-P715	Antiproliferative activity against human OPM-2 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human OPM-2 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
OVCAR-3	IC₅₀	6.202 μM Compound: NMS-P715	Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
OVCAR-8	IC₅₀	1.212 μM Compound: NMS-P715	Antiproliferative activity against human OVCAR-8 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human OVCAR-8 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
PC-3	IC₅₀	1.992 μM Compound: NMS-P715	Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
RERF-LC-AI	IC₅₀	2.068 μM Compound: NMS-P715	Antiproliferative activity against human RERF-LC-AI cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human RERF-LC-AI cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
RO82-W-1	IC₅₀	9.308 μM Compound: NMS-P715	Antiproliferative activity against human RO82-W-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human RO82-W-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
RPMI-8226	IC₅₀	1.484 μM Compound: NMS-P715	Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
SET-2	IC₅₀	10 μM Compound: NMS-P715	Antiproliferative activity against human SET2 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SET2 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
SF-268	IC₅₀	1.372 μM Compound: NMS-P715	Antiproliferative activity against human SF-268 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SF-268 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
SF-295	IC₅₀	2.881 μM Compound: NMS-P715	Antiproliferative activity against human SF-295 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SF-295 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
SF-539	IC₅₀	0.807 μM Compound: NMS-P715	Antiproliferative activity against human SF-539 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SF-539 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
Sf9	IC₅₀	0.007 μM Compound: 5, NMS-P715	Inhibition of N-terminal 6XHis-tagged/GST-tagged full length human MPS1 expressed in recombinant baculovirus infected sf9 insect cells using 5FAM-DHTGFLTEYVATRCONH2 as substrate after 60 to 90 mins by fluorescence assay Inhibition of N-terminal 6XHis-tagged/GST-tagged full length human MPS1 expressed in recombinant baculovirus infected sf9 insect cells using 5FAM-DHTGFLTEYVATRCONH2 as substrate after 60 to 90 mins by fluorescence assay	[PMID: 24256217]
SK-LU-1	IC₅₀	5.002 μM Compound: NMS-P715	Antiproliferative activity against human SK-LU-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SK-LU-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
SKM-1	IC₅₀	10 μM Compound: NMS-P715	Antiproliferative activity against human SKM-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SKM-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
SK-MEL-2	IC₅₀	1.492 μM Compound: NMS-P715	Antiproliferative activity against human SK-MEL-2 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SK-MEL-2 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
SK-MEL-28	IC₅₀	2.594 μM Compound: NMS-P715	Antiproliferative activity against human SK-MEL-28 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SK-MEL-28 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
SK-MEL-5	IC₅₀	4.486 μM Compound: NMS-P715	Antiproliferative activity against human SK-MEL-5 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SK-MEL-5 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
SK-OV-3	IC₅₀	4.258 μM Compound: NMS-P715	Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
SN12C	IC₅₀	1.225 μM Compound: NMS-P715	Antiproliferative activity against human SN12C cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SN12C cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
SNB-19	IC₅₀	6.928 μM Compound: NMS-P715	Antiproliferative activity against human SNB-19 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SNB-19 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
SNB-75	IC₅₀	2.202 μM Compound: NMS-P715	Antiproliferative activity against human SNB-75 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SNB-75 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
SR	IC₅₀	6.959 μM Compound: NMS-P715	Antiproliferative activity against human SR cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SR cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
SUD4	IC₅₀	1.605 μM Compound: NMS-P715	Antiproliferative activity against human SU-DHL-4 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SU-DHL-4 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
SU-DHL-1	IC₅₀	3.309 μM Compound: NMS-P715	Antiproliferative activity against human SU-DHL-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SU-DHL-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
SU-DHL10	IC₅₀	1.579 μM Compound: NMS-P715	Antiproliferative activity against human SU-DHL-10 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SU-DHL-10 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
SU-DHL-6	IC₅₀	10 μM Compound: NMS-P715	Antiproliferative activity against human SU-DHL-6 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SU-DHL-6 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
SU-DHL-8	IC₅₀	0.829 μM Compound: NMS-P715	Antiproliferative activity against human SU-DHL-8 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SU-DHL-8 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
SW1417	IC₅₀	8.842 μM Compound: NMS-P715	Antiproliferative activity against human SW1417 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SW1417 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
SW48	IC₅₀	0.551 μM Compound: NMS-P715	Antiproliferative activity against human SW48 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SW48 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
SW480	IC₅₀	1.298 μM Compound: NMS-P715	Antiproliferative activity against human SW480 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SW480 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
SW-620	IC₅₀	0.472 μM Compound: NMS-P715	Antiproliferative activity against human SW620 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SW620 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
SW948	IC₅₀	1.955 μM Compound: NMS-P715	Antiproliferative activity against human SW948 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SW948 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
T47D	IC₅₀	2.864 μM Compound: NMS-P715	Antiproliferative activity against human T47D cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human T47D cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
T84	IC₅₀	10 μM Compound: NMS-P715	Antiproliferative activity against human T84 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human T84 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
T98G	IC₅₀	0.203 μM Compound: NMS-P715	Antiproliferative activity against human T98G cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human T98G cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
TF-1	IC₅₀	6.526 μM Compound: NMS-P715	Antiproliferative activity against human TF-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human TF-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
TK-10	IC₅₀	1.539 μM Compound: NMS-P715	Antiproliferative activity against human TK-10 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human TK-10 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
Toledo	IC₅₀	1.72 μM Compound: NMS-P715	Antiproliferative activity against human Toledo cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human Toledo cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
U-251	IC₅₀	1.821 μM Compound: NMS-P715	Antiproliferative activity against human U-251 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human U-251 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
U-266	IC₅₀	5.926 μM Compound: NMS-P715	Antiproliferative activity against human U-266 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human U-266 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
U2OS	IC₅₀	0.032 μM Compound: 15, NMS-P715	Inhibition of mitosis in human U2OS cells assessed as histone H3 phosphorylation at Ser 10 residue after 2 hrs by immunoassay Inhibition of mitosis in human U2OS cells assessed as histone H3 phosphorylation at Ser 10 residue after 2 hrs by immunoassay	[PMID: 21723120]
U2OS	IC₅₀	153 nM Compound: Chemical probe: NMS-P715	Antiproliferative activity against human U2OS cells assessed as reduction in cell viability incubated for 5 days Antiproliferative activity against human U2OS cells assessed as reduction in cell viability incubated for 5 days	[PMID: 26364596]
U2OS	IC₅₀	2.09 μM Compound: NMS-P715	Antiproliferative activity against human U2OS cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human U2OS cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
UACC-257	IC₅₀	1.866 μM Compound: NMS-P715	Antiproliferative activity against human UACC-257 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human UACC-257 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
UACC-62	IC₅₀	4.751 μM Compound: NMS-P715	Antiproliferative activity against human UACC-62 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human UACC-62 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]
UO-31	IC₅₀	3.616 μM Compound: NMS-P715	Antiproliferative activity against human UO-31 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human UO-31 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 21159646]

In Vitro

NMS-P715 is a selective inhibitor of MPS1, with an IC₅₀ of 182 nM. NMS-P715 is highly specific for MPS1, with no other kinases inhibited below an IC₅₀ value of 5 μM and only 3 kinases inhibited below 10 μM (CK2, MELK, and NEK6). NMS-P715 promotes massive spindle assembly checkpoint (SAC) override with an EC₅₀ of 65 nM. NMS-P715 (1 μM) causes mitotic acceleration in U2OS cells overexpressing YFP-α-tubulin, induces aneuploidy and inhibits the proliferation of HCT116 cells. NMS-P715 (0.5, 1 μM) affects mitotic checkpoint complex (MCC) stability and cdc20 ubiquitylation^[1]. NMS-P715 (1 μM) exhibits bypass of the spindle assembly checkpoint and apoptosis in pancreatic ductal adenocarcinoma (PDAC) cell lines. NMS-P715 (0-25 μM) also selectively inhibits growth of PDAC cells^[2].

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

In Vivo

NMS-P715 (10 mg/kg) exhibits an oral bioavailability of 37% and good pharmacokinetic properties in nude mice bearing subcutaneous implanted human tumor cell xenografts. NMS-P715 (90 mg/kg, p.o.) is well tolerated and cuases no signs of body weight loss or other overt toxicities in an A2780 ovary carcinoma xenograft model. NMS-P715 (100 mg/kg, p.o.) inhibits the tumor growth by appr 43% in the A375 melanoma xenograft model^[1].

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

Chemical Information

CAS. Nr. 1202055-32-0
Appearance Solid
Molecular Weight 676.73
Formel C₃₅H₃₉F₃N₈O₃
Color White to off-white
SMILES

O=C(C1=NN(C)C2=C1CCC3=C2N=C(NC4=CC=C(C(NC5CCN(CC5)C)=O)C=C4OC(F)(F)F)N=C3)NC6=C(CC)C=CC=C6CC
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 2 mg/mL (2.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

1.4777 mL

7.3885 mL

14.7769 mL

5 mM

---

10 mM

---

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: 0.5% CMC/saline water

Solubility: 3.33 mg/mL (4.92 mM); Suspended solution; Need ultrasonic

Protokoll

Kinase Assay^[1]

The potency of the compound towards MPS1 and 60 additional kinases belonging to kinase selectivity screening (KSS) panel is determined using either a strong anion exchanger based assay or P81 Multiscreen plate. MPS1 activity is measured using 5 nM of MPS1 recombinant protein in 50 mM HEPES pH 7.5, 2.5 mM MgCl₂, 1 mM MnCl₂, 1 mM DTT, 3 μM NaVO₃, 2 mM β-glycerophosphate, 0.2 mg/mL BSA, 200 μM P38-βtide substrate-peptide (KRQADEEMTGYVATRWYRAE) and 8 μM ATP with 1.5 nM ³³P-γ-ATP. The assay is run in a robotized format, 10 serial 1:3 compounds dilutions (including NMS-P715, from 30 μM to 1.5 nM) are tested and IC₅₀ determined^[1].

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

Cell Assay^[1]

Cells lines are seeded in 384 well-plates in the appropiate complete medium and treated with compounds (NMS-P715, etc.) dissolved in 0.1% DMSO 24 hours after seeding. The cells are incubated at 37°C and 5% CO₂ and after 72 hours the plates are processed using CellTiter-Glo assay. Inhibitory activity is evaluated comparing treated versus control data using Assay Explorer software. IC₅₀ of proliferation is calculated using sigmoidal interpolation curve fitting. Activity Ratio is calculated as the ratio of the single cell line IC₅₀ and the IC₅₀ average of all the cell lines tested^[1].

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

Animal Administration^[1]

Mice^[1]
Athymic nu-nu mice, 5-6 weeks of age (20-22 g) are used in the assay. A2780 ovary carcinoma and A375 melanoma cells are transplanted s.c. into female nu-nu mice. Mice bearing a palpable tumor (100-200 mm³) are selected and randomized into control and treated groups. Treatment starts one day after randomization. NMS-P715 is typically administered by oral administration at doses of 90-100 mg/kg daily for more than seven days. Each group includs 8 animals. Tumor dimension is measured regularly by calipers during the experiments and tumor mass is calculated^[1].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)

Verweise

[1]. Colombo R, et al. Targeting the mitotic checkpoint for cancer therapy with NMS-P715, an inhibitor of MPS1 kinase. Cancer Res. 2010 Dec 15;70(24):10255-64. [Content Brief]

[2]. Slee RB, et al. Selective inhibition of pancreatic ductal adenocarcinoma cell growth by the mitotic MPS1 kinase inhibitor NMS-P715. Mol Cancer Ther. 2014 Feb;13(2):307-315. [Content Brief]

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	1.4777 mL	7.3885 mL	14.7769 mL	36.9424 mL

Keywords

Produktname:
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Produktname:
CAS. Nr.:
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NMS-P715

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Targeted Diversity Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NMS-P715

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Targeted Diversity Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NMS-P715 Related Classifications

HY-12382 Related Classifications