NMS-P715

Name: NMS-P715
Brand: MedChemExpress
SKU: HY-12382
Rating: 4.5 (1 reviews)

Cat. No.: HY-12382 Purity: 98.41%: FAQs
Data Sheet SDS COA Handling Instructions

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

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

NMS-P715 Chemical Structure

CAS No. : 1202055-32-0

Size	Price	Stock	Quantity
1 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 190	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1008	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1680	In-stock	Estimated Time of Arrival: December 31
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500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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Description

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
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]
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]
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	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]
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]
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]

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.

Molecular Weight

676.73

Formula

C₃₅H₃₉F₃N₈O₃

CAS No.

1202055-32-0

Appearance

Solid

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

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

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.4777 mL	7.3885 mL	14.7769 mL
5 mM	---	---	---
10 mM	---	---	---

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:

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

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.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.41%

Select Batch:

Data Sheet (276 KB) SDS (393 KB)

COA (248 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[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]

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

Complete Stock Solution Preparation Table

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

NMS-P715 Related Classifications

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:

NMS-P7151202055-32-0Mps1Monopolar spindle 1Inhibitorinhibitorinhibit

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