製品番号: HY-13252

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MK-5108

(別名: VX-689)

7 Cited Publications

カスタマーレビュー

Based on 7 publication(s) in Google Scholar

MK-5108 is a highly potent and specific inhibitor of Aurora A kinase with an IC₅₀ value of 0.064 nM.

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純度: 99.60%
CAS 番号: 1010085-13-8
分子式: C₂₂H₂₁ClFN₃O₃S
分子量:461.94

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

MK-5108 構造式

CAS 番号: 1010085-13-8

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Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (7)
溶剤 & 溶解度
- 体外
- 体内
プロトコル
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

MK-5108 is a highly potent and specific inhibitor of Aurora A kinase with an IC₅₀ value of 0.064 nM.

IC₅₀ & Target^[1]

Aurora A

64 pM (IC₅₀)

Aurora Kinase アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
786-0	IC₅₀	>30 μM Compound: MK-5108	Cytotoxicity against human 786-0 cells measured after 72 hrs by MTT assay Cytotoxicity against human 786-0 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
A673	IC₅₀	>30 μM Compound: MK-5108	Cytotoxicity against human A673 cells measured after 72 hrs by MTT assay Cytotoxicity against human A673 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
AU565	IC₅₀	0.45 μM Compound: 65; VX-689, MK5108	Antiproliferation activity against human AU565 cells assessed as inhibition of cell proliferation Antiproliferation activity against human AU565 cells assessed as inhibition of cell proliferation	[PMID: 28918096]
CAKI-1	IC₅₀	>30 μM Compound: MK-5108	Cytotoxicity against human CAKI-1 cells measured after 72 hrs by MTT assay Cytotoxicity against human CAKI-1 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
CAL-85-1	IC₅₀	0.74 μM Compound: 65; VX-689, MK5108	Antiproliferation activity against human CAL851 cells assessed as inhibition of cell proliferation Antiproliferation activity against human CAL851 cells assessed as inhibition of cell proliferation	[PMID: 28918096]
HCC1143	IC₅₀	0.42 μM Compound: 65; VX-689, MK5108	Antiproliferation activity against human HCC1143 cells assessed as inhibition of cell proliferation Antiproliferation activity against human HCC1143 cells assessed as inhibition of cell proliferation	[PMID: 28918096]
HCC1806	IC₅₀	0.56 μM Compound: 65; VX-689, MK5108	Antiproliferation activity against human HCC1806 cells assessed as inhibition of cell proliferation Antiproliferation activity against human HCC1806 cells assessed as inhibition of cell proliferation	[PMID: 28918096]
HCT-116	IC₅₀	16.3 μM Compound: MK-5108	Cytotoxicity against human HCT-116 cells measured after 72 hrs by MTT assay Cytotoxicity against human HCT-116 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
IGROV-1	IC₅₀	>30 μM Compound: MK-5108	Cytotoxicity against human IGROV-1 cells measured after 72 hrs by MTT assay Cytotoxicity against human IGROV-1 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
IMR-32	IC₅₀	199.2 nM Compound: MK-5108	Antiproliferative activity against human IMR-32 cells assessed as reduction in cell viability incubated for 48 hrs Antiproliferative activity against human IMR-32 cells assessed as reduction in cell viability incubated for 48 hrs	[PMID: 36549117]
MCF7	IC₅₀	>30 μM Compound: MK-5108	Cytotoxicity against human MCF7 cells measured after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
MCF7	IC₅₀	0.52 μM Compound: 65; VX-689, MK5108	Antiproliferation activity against human MCF7 cells assessed as inhibition of cell proliferation Antiproliferation activity against human MCF7 cells assessed as inhibition of cell proliferation	[PMID: 28918096]
NCI-H69	IC₅₀	>30 μM Compound: MK-5108	Cytotoxicity against human NCI-H69 cells measured after 72 hrs by MTT assay Cytotoxicity against human NCI-H69 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
NCI-H82	IC₅₀	>30 μM Compound: MK-5108	Cytotoxicity against human NCI-H82 cells measured after 72 hrs by MTT assay Cytotoxicity against human NCI-H82 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
PC-3	IC₅₀	>30 μM Compound: MK-5108	Cytotoxicity against human PC-3 cells measured after 72 hrs by MTT assay Cytotoxicity against human PC-3 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
Rec1	IC₅₀	>30 μM Compound: MK-5108	Cytotoxicity against human REC1 cells measured after 72 hrs by MTT assay Cytotoxicity against human REC1 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
SK-N-MC	IC₅₀	>30 μM Compound: MK-5108	Cytotoxicity against human SK-N-MC cells measured after 72 hrs by MTT assay Cytotoxicity against human SK-N-MC cells measured after 72 hrs by MTT assay	[PMID: 34624821]
TC-32	IC₅₀	5.6 μM Compound: MK-5108	Cytotoxicity against human TC-32 cells measured after 72 hrs by MTT assay Cytotoxicity against human TC-32 cells measured after 72 hrs by MTT assay	[PMID: 34624821]

体外実験

MK-5108 inhibits Aurora-A activity with an IC₅₀ value of 0.064 nM in an ATP-competitive manner. It shows robust selectivity against the other family kinases Aurora-B (220-fold) and Aurora-C (190-fold). MK-5108 also exhibits high selectivity for Aurora-A over other protein kinases. MK-5108 inhibits the growth of 14 cell lines with IC₅₀ values between 0.16 and 6.4 μM^[1].

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

体内実験

MK-5108 treatments at 15 and 30 mg/kg results in significant tumor growth inhibition in the HCT116 tumor model. MK-5108 is well tolerated at both doses, with minimal reduction in body weight. MK-5108 also exhibits significant antitumor activity in nude rats bearing SW48 tumors. MK-5108 at 15 and 45 mg/kg causes dose-dependent tumor growth inhibition with a %T/C of 35% and 7% at day 10, and 58% and 32% at day 27, respectively. MK-5108 is well tolerated in nude rats, with no body weight reduction and moderate effect on blood cells^[1].

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

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 1010085-13-8
性状 Solid
分子量 461.94
分子式 C₂₂H₂₁ClFN₃O₃S
Color White to off-white
SMILES

FC(C(Cl)=CC=C1)=C1O[C@H](CC2)CC[C@@]2(C(O)=O)CC3=CC=CC(NC4=NC=CS4)=N3
別名

VX-689
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (7)

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Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Sci Adv

Phosphorylation by Aurora kinase A facilitates cortical-cytoplasmic dynamics of Par-3 in asymmetric division of radial glia progenitors. [Abstract]

2025 May 16;11(20):eadq3858. PMID: 40367180
Cell Rep Methods

A hybrid deep forest-based method for predicting synergistic drug combinations. [Abstract]

2023 Feb 21;3(2):100411. PMID: 36936075
bioRxiv

2026 Apr 18.
University of California

2024.
Patent

US20180263995A1.
Technical University of Munich

24.01.2018.

溶剤 & 溶解度

体外:

DMSO : 12.5 mg/mL (27.06 mM; ultrasonic and warming and heat to 60°C; 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

2.1648 mL

10.8239 mL

21.6478 mL

5 mM

0.4330 mL

2.1648 mL

4.3296 mL

10 mM

0.2165 mL

1.0824 mL

2.1648 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

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: ≥ 1.25 mg/mL (2.71 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (2.71 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.25 mg/mL (2.71 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 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 (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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% Methyl cellulose/0.5% Tween-80 in Saline water

Solubility: 6.67 mg/mL (14.44 mM); Suspended solution; Need ultrasonic

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

プロトコル

Kinase Assay^[1]

The Aurora-A assay reaction is conducted in the presence of 20 μM ATP, 25 μM Tetra-Kemptide, 1.0 μCi per well [γ-³³P]-ATP, 0.1 ng per well Aurora-A in 50 mmol/L Tris-HCl (pH 7.4), 15 mmol/L Mg(OAc)₂, and 0.2 mmol/L EDTA at 30°C for 40 min. To investigate the inhibition mode of MK-5108 for Aurora-A, the IC₅₀ values of MK-5108 are determined in the presence of different concentrations of ATP. Then, the IC₅₀ value is plotted as a function of ATP concentration to analyze the effect of ATP concentration on the IC₅₀ value of MK-5108^[1].

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

Cell Assay^[1]

Cells are seeded in 96-well plates then incubated overnight. A medium containing MK-5108, docetaxel, or DMSO control is added and is incubated for 72 h. The cell population densities are then measured by the WST-8 colorimetric assay using a SpectraMax Plus384 plate reader. Concentration response curves are generated to give the decrease in cell population density in MK-5108– and docetaxel-treated samples relative to DMSO-treated control. Growth inhibition IC₅₀ values are determined from those curves^[1].

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

Animal Administration^[1]

Rats: After 8 d, MK-5108 is suspended in 0.5% methyl cellulose/0.24% SDS and orally administered twice daily for 14 d. SW48 cells are suspended in 50% Matrigel/50% PBS and s.c. transplanted into the side flank of nude rats. After 7 d, MK-5108 is suspended in 0.5% methyl cellulose/0.24% SDS and orally administered twice daily for 2 d/wk for 3 wk. In a HeLa-luc and ES-2 dual flank xenograft model, HeLa-luc or ES-2 cells are suspended in 50% Matrigel and 50% PBS, and s.c. transplanted into the right or left side flank of nude rats. After 8 d, vehicle (5% ethanol-saline) or 7.5 mg/kg docetaxel is injected i.v. MK-5108 is orally administered twice daily for 2 d 24 h after the docetaxel injection. The volume of each tumor is determined from the tumor diameter^[1].

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[1]. Shimomura T, et al. MK-5108, a highly selective Aurora-A kinase inhibitor, shows antitumor activity alone and in combination with docetaxel. Mol Cancer Ther. 2010 Jan;9(1):157-66. [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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1648 mL	10.8239 mL	21.6478 mL	54.1196 mL
	5 mM	0.4330 mL	2.1648 mL	4.3296 mL	10.8239 mL
	10 mM	0.2165 mL	1.0824 mL	2.1648 mL	5.4120 mL
	15 mM	0.1443 mL	0.7216 mL	1.4432 mL	3.6080 mL
	20 mM	0.1082 mL	0.5412 mL	1.0824 mL	2.7060 mL
	25 mM	0.0866 mL	0.4330 mL	0.8659 mL	2.1648 mL

Keywords

MK-5108

7 Cited Publications

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MK-5108

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

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Anti-Aging Compound Library

Cytoskeleton Compound Library

Chemical Probe Library

Anti-Blood Cancer Compound Library

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Highly Selective Activators Library

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Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

MedChemExpress（MCE）の使用を引用している文献 MK-5108

Aurora Kinase アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (7)

溶剤 & 溶解度

プロトコル

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

MK-5108

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Chemical Probe Library

Anti-Blood Cancer Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

MedChemExpress（MCE）の使用を引用している文献 MK-5108

Aurora Kinase アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (7)

溶剤 & 溶解度

プロトコル

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

MK-5108 関連分類

製品番号: HY-13252