Cat. No.: HY-14710

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AZ3146

11 Cited Publications

Customer Review

Based on 11 publication(s) in Google Scholar

AZ3146 is a reasonably potent Mps1 and TTK inhibitor, with IC₅₀ of 35 nM for Mps1^Cat.

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

Purity: 99.42%
CAS No.: 1124329-14-1
Formula: C₂₄H₃₂N₆O₃
Molecular Weight:452.55

Storage:

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

AZ3146 Chemical Structure

CAS No.: 1124329-14-1

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (11)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

AZ3146 is a reasonably potent Mps1 and TTK inhibitor, with IC₅₀ of 35 nM for Mps1^Cat.

IC₅₀ & Target^[1]

Mps1^Cat

35 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
DLD-1	IC₅₀	>5000 nM Compound: Chemical probe: AZ3146	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	719 nM Compound: Chemical probe: AZ3146	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]
HCT-116	GI₅₀	1.2 μM Compound: 4, AZ3146	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	>5000 nM Compound: Chemical probe: AZ3146	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	0.72 μM Compound: 4, AZ3146	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	3063 nM Compound: Chemical probe: AZ3146	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	560 nM Compound: Chemical probe: AZ3146	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]
HeLa	IC₅₀	>5000 nM Compound: Chemical probe: AZ3146	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	1335 nM Compound: Chemical probe: AZ3146	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	2743 nM Compound: Chemical probe: AZ3146	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	3847 nM Compound: Chemical probe: AZ3146	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]
MDA-MB-468	IC₅₀	2.101 μM Compound: 5; AZ-3146	Antiproliferative activity against human MDA-MB-468 cells assessed inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MDA-MB-468 cells assessed inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37037136]
Sf9	IC₅₀	0.007 μM Compound: 4, AZ3146	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]

In Vitro

In in vitro kinase assays, AZ3146 inhibits human Mps1^Cat with IC₅₀ of ~35 nM. AZ3146 also efficiently inhibits autophosphorylation of full-length Mps1 immunoprecipitated from human cells^[1].
TTK specific kinase inhibitor AZ3146 can decrease HCC cell growth. In vitro cell cytotoxicity assays are performed on SMMC-7721 and BEL-7404 cells. IC₅₀s are calculated as being 7.13 μM (BEL-7404) and 28.62 μM (SMMC-7721). Both cells are further treated under the concentration of IC50 for 4 days. Significant inhibitions of cell proliferation are observed^[2].
HCT116 cells are cultured for 10 days in 0.8 μM (the GI₅₀) of AZ3146 , then 2 μM AZ3146 for 3 weeks. Sixteen clones are isolated and cell lines generated, named AzR1-16, all of which are resistant to AZ3146-induced cell death in cell viability assays; AzR3 and 4 have a GI₅₀ of approximately 3 μM (4-fold resistance), while the remaining clones have a GI₅₀ of approximately 9 μM (11-fold resistance). When analyzing mitosis by time-lapse microscopy, while 2 μM AZ3146 causes the parental cell line to rapidly exited mitosis in 10 minutes^[3].

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

Chemical Information

CAS No. 1124329-14-1
Appearance Solid
Molecular Weight 452.55
Formula C₂₄H₃₂N₆O₃
Color Off-white to light yellow
SMILES

CN(CC1)CCC1OC2=CC=C(NC3=NC(N(C4CCCC4)C(N5C)=O)=C5C=N3)C(OC)=C2
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

Publications (11)

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Nat Cell Biol

Chromosome mis-segregation triggers cell cycle arrest through a mechanosensitive nuclear envelope checkpoint. [Abstract]

2025 Jan;27(1):73-86. PMID: 39779939
Nat Commun

Polar chromosomes are rescued from missegregation by spindle elongation-driven microtubule pivoting. [Abstract]

2026 Mar 17;17(1):2049. PMID: 41844586
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Acta Pharmacol Sin

Chromosome instability functions as a potential therapeutic reference by enhancing chemosensitivity to BCL-XL inhibitors in colorectal carcinoma. [Abstract]

2024 Nov;45(11):2420-2431. PMID: 39187678
J Genet Genomics

SYMPK interacts with KIF20A and NUMA1 to coordinate spindle organization and safeguard oocyte meiotic maturation. [Abstract]

2026 Jan 9:S1673-8527(26)00002-0. PMID: 41520922
Mol Oncol

Repositioning VU-0365114 as a novel microtubule-destabilizing agent for treating cancer and overcoming drug resistance. [Abstract]

2024 Feb;18(2):386-414. PMID: 37842807
J Biol Chem

Aurora B kinase activity-dependent and -independent functions of the chromosomal passenger complex in regulating sister chromatid cohesion. [Abstract]

2019 Feb 8;294(6):2021-2035. PMID: 30523151
bioRxiv

2025 March 06.
bioRxiv

2025 March 19.
bioRxiv

2024 June 16.
bioRxiv

September 11, 2018.

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (220.97 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

2.2097 mL

11.0485 mL

22.0970 mL

5 mM

0.4419 mL

2.2097 mL

4.4194 mL

10 mM

0.2210 mL

1.1049 mL

2.2097 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, 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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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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 (5.52 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 (5.52 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 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

Protocol

Kinase Assay^[1]

His-tagged human Mps1^Cat encoding amino acids 510-857 is generated. For kinase assays, 500 ng is added to buffer (25 mM Tris-HCl, pH 7.4, 100 mM NaCl, 50 µg/mL BSA, 0.1 mM EGTA, 0.1% β-mercaptoethanol, 10 mM MgCl₂, and 0.5 µg/mL myelin basic protein), AZ3146, and 100 µM γ-[³²P]ATP (2 µCi/assay). Reactions are incubated at 30°C for 20 min, spotted onto P81 paper, washed in 0.5% phosphoric acid, and immersed in acetone. Phosphate incorporation is determined by scintillation counting. For immunoprecipitation kinase assays, HeLa cells are treated with nocodazole for 14 h, mitotic cells isolated, washed in PBS, and lysed for 30 min in 50 mM Tris-HCl, pH 7.4, 100 mM NaCl, 0.5% NP-40, 5 mM EDTA, 5 mM EGTA, 40 mM β-glycerophosphate, 0.2 mM PMSF, 1 mM DTT, 1 mM sodium orthovanadate, 20 mM sodium fluoride, 1 µM okadaic acid, and complete EDTA-free protease inhibitor cocktail. Full-length Mps1 is immunoprecipitated. Purified complexes are washed with lysis buffer containing 100 mM NaCl and assayed as described for the recombinant protein. To quantify ³²P incorporation, reactions are stopped with SDS sample buffer and separated by SDS-PAGE followed by phosphorimaging. The plate is analyzed using a phosphorimager using AIDA software. To assess the specificity of AZ3146, a single-point screen is carried using kinase profiling service. 50 kinases are selected and assayed with 1 µM AZ3146^[1].

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

Cell Assay^[2]

The TTK inhibitor AZ3146 is disolved in DMSO at a concentration in 100 mM and diluted into 100 μM, 10 μM, 1 μM and 0.1 μM sequentially with DMEM containing 10% FBS before use. In vitrocytotoxicity assays are performed. HCC cells are plated into 96-well plates at the density of 3×10³ per well. AZ3146 is added in the indicated concentrations the next day. The inhibitor treated cells are cultured and tested at a 24-hour intervals for 3-4 days using CCK-8^[2].

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 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)
- 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)

References

[1]. Hewitt L, et al. Sustained Mps1 activity is required in mitosis to recruit O-Mad2 to the Mad1-C-Mad2 core complex. J Cell Biol. 2010 Jul 12;190(1):25-34. [Content Brief]

[2]. Liu X, et al. TTK activates Akt and promotes proliferation and migration of hepatocellular carcinoma cells. Oncotarget. 2015 Oct 27;6(33):34309-20. [Content Brief]

[3]. Gurden MD, et al. Naturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug Resistance. Cancer Res. 2015 Aug 15;75(16):3340-54. [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	2.2097 mL	11.0485 mL	22.0970 mL	55.2425 mL
	5 mM	0.4419 mL	2.2097 mL	4.4194 mL	11.0485 mL
	10 mM	0.2210 mL	1.1049 mL	2.2097 mL	5.5243 mL
	15 mM	0.1473 mL	0.7366 mL	1.4731 mL	3.6828 mL
	20 mM	0.1105 mL	0.5524 mL	1.1049 mL	2.7621 mL
	25 mM	0.0884 mL	0.4419 mL	0.8839 mL	2.2097 mL
	30 mM	0.0737 mL	0.3683 mL	0.7366 mL	1.8414 mL
	40 mM	0.0552 mL	0.2762 mL	0.5524 mL	1.3811 mL
	50 mM	0.0442 mL	0.2210 mL	0.4419 mL	1.1049 mL
	60 mM	0.0368 mL	0.1841 mL	0.3683 mL	0.9207 mL
	80 mM	0.0276 mL	0.1381 mL	0.2762 mL	0.6905 mL
	100 mM	0.0221 mL	0.1105 mL	0.2210 mL	0.5524 mL

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AZ3146

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) AZ3146

Biological Activity

Chemical Information

Publications (11)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

AZ3146

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) AZ3146

Biological Activity

Chemical Information

Publications (11)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

AZ3146 Related Classifications

Cat. No.: HY-14710