Art. -Nr.: HY-12401

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Mps1-IN-3

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Mps1-IN-3 is a potent and selective MPS1 kinase inhibitor, with an IC₅₀ of 50 nM.

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Reinheit: 99.73%
CAS. Nr.: 1609584-72-6
Formel: C₂₆H₃₁N₇O₄S
Molecular Weight:537.63

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Mps1-IN-3 Chemical Structure

CAS. Nr.: 1609584-72-6

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Mps1-IN-3 is a potent and selective MPS1 kinase inhibitor, with an IC₅₀ of 50 nM.

IC₅₀ & Target^[1]

Mps1

50 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
DLD-1	IC₅₀	2415 nM Compound: Chemical probe: Mps1-IN-3	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]
DLD-1	IC₅₀	7931 nM Compound: Chemical probe: Mps1-IN-3	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]
HCT-116	IC₅₀	1624 nM Compound: Chemical probe: Mps1-IN-3	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	3234 nM Compound: Chemical probe: Mps1-IN-3	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	5403 nM Compound: Chemical probe: Mps1-IN-3	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]
HeLa	IC₅₀	3417 nM Compound: Chemical probe: Mps1-IN-3	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	4793 nM Compound: Chemical probe: Mps1-IN-3	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	6793 nM Compound: Chemical probe: Mps1-IN-3	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	8974 nM Compound: Chemical probe: Mps1-IN-3	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]

In Vitro

Mps1-IN-3 is a potent MPS1 kinase inhibitor, with an IC₅₀ of 50 nM. Mps1-IN-3 inhibits the proliferation of U251 glioblastoma cells with an IC₅₀ of appr 5 µM. Mps1-IN-3 (2 μM) can completely abrogates checkpoint^[1].

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

In Vivo

Mps1-IN-3 (2 mg/kg, i.v.) sensitizes glioblastoma cells in murine tumor models, with prolonged survival and no toxicity^[1].

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

Chemical Information

CAS. Nr. 1609584-72-6
Appearance Solid
Molecular Weight 537.63
Formel C₂₆H₃₁N₇O₄S
Color White to light brown
SMILES

OC1CCN(C2=CC=C(NC3=NC(NC4=CC=CC=C4S(=O)(C(C)C)=O)=C5N=CNC5=N3)C(OC)=C2)CC1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Cell Metab

Creatine promotes cancer metastasis through activation of Smad2/3. [Abstract]

2021 Jun 1;33(6):1111-1123.e4. PMID: 33811821

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (186.00 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

1.8600 mL

9.3001 mL

18.6002 mL

5 mM

0.3720 mL

1.8600 mL

3.7200 mL

10 mM

0.1860 mL

0.9300 mL

1.8600 mL

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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:

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

Stock Solution Working Solution

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 (4.65 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (4.65 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protokoll

Animal Administration^[1]

Mice^[1]
Six-week old athymic female nude mice weighing about 25 g are stereotactically injected with 1 × 10⁶ U251-FM-shCTRL or shMPS1 cells, or U251-FM, or 3 × 10⁵ GBM8-FM cells (in 10 and 4 μL PBS, respectively) using a stereotactic instrument after drilling a small hole in the cranium of the mice. For the U251-FM-shRNA experiment, a minimum of 3 mice per group is used, and for the U251-FM and GBM8-FM cells, at least 5 mice per group are used. Tumor growth is monitored by Fluc bioluminescence imaging after injection of 150 μL D-luciferin (50 mg/mL) and imaging 10 min later for luciferase-mediated photon activity using the IVIS Lumina imaging system for the U251-FM model and the IVIS Spectrum for the GBM8-FM model. When tumors reach a size around 10⁷ radiance for the U251 model and 5 × 10⁵ radiance for the GBM8 model, mice are intravenously injected with vehicle, and/or 2 mg/kg MPS1-IN-3 in 20% hydroxypropyl-beta-cyclodextrin (HPbetaCD), twice/week over three weeks. Tumor volume is monitored weekly by Fluc imaging^[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 (278 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]. Tannous BA, et al. Effects of the selective MPS1 inhibitor MPS1-IN-3 on glioblastoma sensitivity to antimitotic drugs. J Natl Cancer Inst. 2013 Sep 4;105(17):1322-31. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8600 mL	9.3001 mL	18.6002 mL	46.5004 mL
	5 mM	0.3720 mL	1.8600 mL	3.7200 mL	9.3001 mL
	10 mM	0.1860 mL	0.9300 mL	1.8600 mL	4.6500 mL
	15 mM	0.1240 mL	0.6200 mL	1.2400 mL	3.1000 mL
	20 mM	0.0930 mL	0.4650 mL	0.9300 mL	2.3250 mL
	25 mM	0.0744 mL	0.3720 mL	0.7440 mL	1.8600 mL
	30 mM	0.0620 mL	0.3100 mL	0.6200 mL	1.5500 mL
	40 mM	0.0465 mL	0.2325 mL	0.4650 mL	1.1625 mL
	50 mM	0.0372 mL	0.1860 mL	0.3720 mL	0.9300 mL
	60 mM	0.0310 mL	0.1550 mL	0.3100 mL	0.7750 mL
	80 mM	0.0233 mL	0.1163 mL	0.2325 mL	0.5813 mL
	100 mM	0.0186 mL	0.0930 mL	0.1860 mL	0.4650 mL

Keywords

Mps1-IN-3

1 Cited Publications

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Mps1-IN-3

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Mps1-IN-3

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Mps1-IN-3

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Mps1-IN-3

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Mps1-IN-3 Related Classifications

HY-12401 Related Classifications