Mps1-IN-1

Name: Mps1-IN-1
Brand: MedChemExpress
SKU: HY-13298
Rating: 5.0 (3 reviews)

Cat. No.: HY-13298 Purity: 99.77%: FAQs
Data Sheet SDS COA Handling Instructions

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Mps1-IN-1 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC₅₀ and a K_d of 367 nM and 27 nM.

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

Mps1-IN-1 Chemical Structure

CAS No. : 1125593-20-5

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Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 132	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 132	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 112	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 206	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 726	In-stock	Estimated Time of Arrival: December 31
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Based on 3 publication(s) in Google Scholar

Other Forms of Mps1-IN-1:

Mps1-IN-1 dihydrochloride Get quote

3 Publications Citing Use of MCE Mps1-IN-1

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Protocol
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Description

Mps1-IN-1 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC₅₀ and a K_d of 367 nM and 27 nM^[1].

IC₅₀ & Target^[1]

Mps1

367 nM (IC₅₀)

Mps1

27 nM (Kd)

ALK

21 nM (Kd)

LTK

29 nM (Kd)

PYK2

280 nM (Kd)

FAK

440 nM (Kd)

IGF1R

750 nM (Kd)

INSR

470 nM (Kd)

CLK1

1900 nM (Kd)

ERK2

2900 nM (Kd)

INSRR

1200 nM (Kd)

TNK1

2600 nM (Kd)

TNK2

3100 nM (Kd)

GAK

1100 nM (Kd)

Cellular Effect

Cell Line	Type	Value	Description	References
AU565	IC₅₀	> 10 μM Compound: Mps1-IN-1	Antiproliferative activity against human AU565 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human AU565 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
BT-20	IC₅₀	> 10 μM Compound: Mps1-IN-1	Antiproliferative activity against human BT20 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human BT20 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
BT-474	IC₅₀	> 10 μM Compound: Mps1-IN-1	Antiproliferative activity against human BT474 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human BT474 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
BT-549	IC₅₀	1.73 μM Compound: Mps1-IN-1	Antiproliferative activity against human BT549 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human BT549 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
CAL-51	IC₅₀	2.92 μM Compound: Mps1-IN-1	Antiproliferative activity against human CAL51 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human CAL51 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
CAMA-1	IC₅₀	> 10 μM Compound: Mps1-IN-1	Antiproliferative activity against human CAMA1 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human CAMA1 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
HCC1937	IC₅₀	> 10 μM Compound: Mps1-IN-1	Antiproliferative activity against human HCC1937 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human HCC1937 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
Hs-578T	IC₅₀	> 10 μM Compound: Mps1-IN-1	Antiproliferative activity against human Hs578T cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human Hs578T cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
MCF7	IC₅₀	> 10 μM Compound: Mps1-IN-1	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
MDA-MB-231	IC₅₀	> 10 μM Compound: Mps1-IN-1	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
MDA-MB-436	IC₅₀	> 10 μM Compound: Mps1-IN-1	Antiproliferative activity against human MDA-MB-436 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human MDA-MB-436 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
MDA-MB-453	IC₅₀	> 10 μM Compound: Mps1-IN-1	Antiproliferative activity against human MDA-MB-453 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human MDA-MB-453 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
MDA-MB-468	IC₅₀	1.85 μM Compound: Mps1-IN-1	Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
SK-BR-3	IC₅₀	> 10 μM Compound: Mps1-IN-1	Antiproliferative activity against human SK-BR-3 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human SK-BR-3 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
T47D	IC₅₀	> 10 μM Compound: Mps1-IN-1	Antiproliferative activity against human T47D cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human T47D cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]

In Vitro

Mps1-IN-1 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC₅₀ and a K_d of 367 nM and 27 nM. Mps1-IN-1 also has high affinity for ALK, and LTK, with K_ds of 21 and 39 nM, respectively, but shows little or no inhibition on other 352 member kinases. Mps1-IN-1 (5, 10 μM) induces bypass of a checkpoint-mediated mitotic arrest in U2OS cells. Mps1-IN-1 disrupts recruitment of Mad2 to kinetochores, and reduces the phosphorylation status of Aurora B at threonine-232 (Thr232). Mps1-IN-1 (10 μM) shows no effect on centrosome duplication. In addition, Mps1-IN-1 (5-10 μM) suppresses the proliferative capacity of HCT116^[1].

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

Molecular Weight

535.66

Formula

C₂₈H₃₃N₅O₄S

CAS No.

1125593-20-5

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=S(C(C=CC=C1)=C1NC2=CC(NC3=C(OC)C=C(N4CCC(O)CC4)C=C3)=NC5=C2C=CN5)(C(C)C)=O

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 : ≥ 39 mg/mL (72.81 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8669 mL	9.3343 mL	18.6686 mL
5 mM	0.3734 mL	1.8669 mL	3.7337 mL
10 mM	0.1867 mL	0.9334 mL	1.8669 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.67 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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

Calculation results:

Working solution concentration: mg/mL

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

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

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

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

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

Purity & Documentation

Purity: 99.77%

Select Batch:

Data Sheet (280 KB) SDS (393 KB)

COA (255 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Kwiatkowski N, et al. Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nat Chem Biol. 2010 May;6(5):359-68. [Content Brief]

Kinase Assay ^[1]	The kinase binding assay is used to assess compound binding to TTK by monitoring displacement of a fluorescently labeled, ATP site-directed kinase inhibitor (Kinase Tracer 236) from the kinase active site. Each 15 μL assay contains 5 nM TTK, variable amounts of test compound (Mps1-IN-1), 30 nM Kinase Tracer 236, 2 nM Eu-anti-GST Antibody, and 1% DMSO (residual from compound dilution) in Kinase Buffer A (50 mM HEPES pH 7.5, 10 mM MgCl₂, 1 mM EGTA, 0.01% Brij-35). Binding assays are initiated by addition of 5 μL of test compound (from 2-fold dilution series) to 5 μL of a kinase/antibody mixture, followed by addition of 5 μL of antibody. Assay plates are read using using standard Eu-based TR-FRET settings with excitation at 340 nm and emission monitored at 615 nm (donor) and 665 nm (acceptor). Emission intensities are measured over a 200 µs window following a 100 µs post-excitation delay^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	U2OS cells expressing doxycycline-inducible PLK4 are plated in 96 well plates. A double thymidine block is performed using the following treatment regimen: thymidine for 18-20 hrs., release for 10 hrs. with doxycycline induction of PLK4 during this time, then a second thymidine block, followed by release. Six hours after the 2nd thymidine release, Mps1-IN-1 (or DMSO vehicle) is added and the proliferation of the cell populations is monitored with Cell Titer GLO assay^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Kwiatkowski N, et al. Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nat Chem Biol. 2010 May;6(5):359-68. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.8669 mL	9.3343 mL	18.6686 mL	46.6714 mL
	5 mM	0.3734 mL	1.8669 mL	3.7337 mL	9.3343 mL
	10 mM	0.1867 mL	0.9334 mL	1.8669 mL	4.6671 mL
	15 mM	0.1245 mL	0.6223 mL	1.2446 mL	3.1114 mL
	20 mM	0.0933 mL	0.4667 mL	0.9334 mL	2.3336 mL
	25 mM	0.0747 mL	0.3734 mL	0.7467 mL	1.8669 mL
	30 mM	0.0622 mL	0.3111 mL	0.6223 mL	1.5557 mL
	40 mM	0.0467 mL	0.2334 mL	0.4667 mL	1.1668 mL
	50 mM	0.0373 mL	0.1867 mL	0.3734 mL	0.9334 mL
	60 mM	0.0311 mL	0.1556 mL	0.3111 mL	0.7779 mL

Mps1-IN-1 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:

Mps1-IN-11125593-20-5Mps1Monopolar spindle 1Inhibitorinhibitorinhibit

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Mps1-IN-1

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Other Forms of Mps1-IN-1:

Mps1-IN-1 Related Antibodies

3 Publications Citing Use of MCE Mps1-IN-1

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Biological Activity

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Purity & Documentation

References

Customer Review

Mps1-IN-1 Related Antibodies

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Complete Stock Solution Preparation Table

Mps1-IN-1 Related Classifications

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