Mps1-IN-2

Cat. No.: HY-13994 Purity: 98.04%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Mps1-IN-2 is a potent, selective and ATP-competitive dual Mps1/Plk1 inhibitor, with an IC₅₀ and a K_d of 145 nM and 12 nM for Mps1 and a K_d of 61 nM for Plk1.

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

Mps1-IN-2 Chemical Structure

CAS No. : 1228817-38-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 104	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 104	In-stock	Estimated Time of Arrival: December 31
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5 mg	USD 94	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 175	In-stock	Estimated Time of Arrival: December 31
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PLK1 PLK2 PLK3 PLK4

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Protocol
Purity & Documentation
References
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Description

Mps1-IN-2 is a potent, selective and ATP-competitive dual Mps1/Plk1 inhibitor, with an IC₅₀ and a K_d of 145 nM and 12 nM for Mps1 and a K_d of 61 nM for Plk1.

IC₅₀ & Target^[1]

Mps1

12 nM (Kd)

GAK

140 nM (Kd)

PLK1

61 nM (Kd)

PLK3

1600 nM (Kd)

PLK4

3100 nM (Kd)

STK33

5000 nM (Kd)

In Vitro

Mps1-IN-2 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC₅₀ and a K_d of 145 nM and 12 nM. Mps1-IN-2 also shows high affinity for PLK1 and GAK with K_ds of 61 and 140 nM, respectively, but shows little or no inhibition on other 352 member kinases. Mps1-IN-2 can induces bypass of a checkpoint-mediated mitotic arrest in U2OS cells^[1].

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

Molecular Weight

480.60

Formula

C₂₆H₃₆N₆O₃

CAS No.

1228817-38-6

Appearance

Solid

Color

Light brown to brown

SMILES

CN(C1=CN=C(NC2=C(OCC)C=C(N3CCC(O)CC3)C=C2)N=C1N(C4CCCC4)CC5)C5=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 : 13.33 mg/mL (27.74 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	2.0807 mL	10.4037 mL	20.8073 mL
5 mM	0.4161 mL	2.0807 mL	4.1615 mL
10 mM	0.2081 mL	1.0404 mL	2.0807 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: ≥ 1.33 mg/mL (2.77 mM); Clear solution

This protocol yields a clear solution of ≥ 1.33 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (13.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.33 mg/mL (2.77 mM); Clear solution

This protocol yields a clear solution of ≥ 1.33 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (13.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.33 mg/mL (2.77 mM); Clear solution

This protocol yields a clear solution of ≥ 1.33 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (13.3 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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

Calculation results:

Working solution concentration: mg/mL

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

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

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

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

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

Purity & Documentation

Purity: 98.04%

Select Batch:

Data Sheet (277 KB) SDS (252 KB)

COA (253 KB) LCMS (268 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-2), 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.

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	2.0807 mL	10.4037 mL	20.8073 mL	52.0183 mL
	5 mM	0.4161 mL	2.0807 mL	4.1615 mL	10.4037 mL
	10 mM	0.2081 mL	1.0404 mL	2.0807 mL	5.2018 mL
	15 mM	0.1387 mL	0.6936 mL	1.3872 mL	3.4679 mL
	20 mM	0.1040 mL	0.5202 mL	1.0404 mL	2.6009 mL
	25 mM	0.0832 mL	0.4161 mL	0.8323 mL	2.0807 mL

Mps1-IN-2 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-21228817-38-6Mps1Polo-like Kinase (PLK)Monopolar spindle 1Inhibitorinhibitorinhibit

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Mps1-IN-2

Mps1-IN-2 Related Antibodies

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Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Mps1-IN-2 Related Antibodies

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Complete Stock Solution Preparation Table

Mps1-IN-2 Related Classifications

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