AKI603
Based on 1 Customer Validation
AKI603 is an inhibitor of Aurora kinase A (AurA), with an IC50 of 12.3 nM. AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells.
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- Pureza: 98.03%
- No. CAS: 1432515-73-5
- Fòrmula: C19H23N9O2
- Peso molecular:409.45
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Ver todos los productos específicos de isoformas Aurora Kinase
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Actividad biológica
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Aurora A 12.3 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
0.15 μM
Compound: 7u
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Antiproliferative activity against human A431 cells assessed as cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human A431 cells assessed as cell viability after 72 hrs by CCK8 assay
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[PMID: 24681066] |
| A549 | IC50 |
0.723 μM
Compound: 7u
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Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by CCK8 assay
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[PMID: 24681066] |
| DU-145 | IC50 |
1.2 μM
Compound: 7u
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Antiproliferative activity against human DU145 cells assessed as cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human DU145 cells assessed as cell viability after 72 hrs by CCK8 assay
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[PMID: 24681066] |
| HCT-116 | IC50 |
1.63 μM
Compound: 7u
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Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs by CCK8 assay
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[PMID: 24681066] |
| HeLa | IC50 |
0.331 μM
Compound: 7u
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Antiproliferative activity against human HeLa cells assessed as cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human HeLa cells assessed as cell viability after 72 hrs by CCK8 assay
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[PMID: 24681066] |
| HL-60 | IC50 |
0.0698 μM
Compound: 7u
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Antiproliferative activity against human HL60 cells assessed as cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human HL60 cells assessed as cell viability after 72 hrs by CCK8 assay
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[PMID: 24681066] |
| K562 | IC50 |
0.137 μM
Compound: 7u
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Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CCK8 assay
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[PMID: 24681066] |
| MCF7 | IC50 |
0.424 μM
Compound: 7u
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Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by CCK8 assay
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[PMID: 24681066] |
| MDA-MB-231 | IC50 |
0.0844 μM
Compound: 7u
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Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by CCK8 assay
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[PMID: 24681066] |
| MOLT-4 | IC50 |
0.0181 μM
Compound: 7u
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Antiproliferative activity against human MOLT4 cells assessed as cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human MOLT4 cells assessed as cell viability after 72 hrs by CCK8 assay
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[PMID: 24681066] |
| NCI-N87 | IC50 |
3.88 μM
Compound: 7u
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Antiproliferative activity against human NCI-N87 cells assessed as cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human NCI-N87 cells assessed as cell viability after 72 hrs by CCK8 assay
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[PMID: 24681066] |
| PANC-1 | IC50 |
0.442 μM
Compound: 7u
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Antiproliferative activity against human PANC1 cells assessed as cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human PANC1 cells assessed as cell viability after 72 hrs by CCK8 assay
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[PMID: 24681066] |
| PC-3 | IC50 |
1.09 μM
Compound: 7u
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Antiproliferative activity against human PC3 cells assessed as cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human PC3 cells assessed as cell viability after 72 hrs by CCK8 assay
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[PMID: 24681066] |
| SK-BR-3 | IC50 |
0.437 μM
Compound: 7u
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Antiproliferative activity against human SKBR3 cells assessed as cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human SKBR3 cells assessed as cell viability after 72 hrs by CCK8 assay
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[PMID: 24681066] |
| U-937 | IC50 |
0.0433 μM
Compound: 7u
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Antiproliferative activity against human U937 cells assessed as cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human U937 cells assessed as cell viability after 72 hrs by CCK8 assay
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[PMID: 24681066] |
AKI603 (0.039-0.6 μM; 48 hours) extensively inhibits proliferation of leukemia cells[1].
AKI603 (0.039-0.6 μM; 48 hours) significantly inhibits the phosphorylation of AurA in NB4, K562, and Jurkat cell lines in a dose-dependent manner while the level of total AurA protein is not changed[1].
AKI603 inhibits the proliferation and colony formation of imatinib resistant CML cells[1].
AKI603 (0.3-0.6 μM; 48 hours) inhibits cell proliferation and colony formation capacities in imatinib-resistant CML cells by inducing cell cycle arrest with polyploidy accumulation[1].
Inhibition of AurA by AKI603 induces leukemia cell senescence in both BCR-ABL wild type and T315I mutation cells[1].
AKI603 exhibits inhibitory activities on breast cancer cell proliferation, such as SUM149 (IC50=2.04), BT549 (IC50=0.86), MCF-7 (IC50=0.97), MCF-7-Epi (IC50=21.01), Sk-br-3 (IC50=0.73), MDA-MB-231 (IC50=3.49), MDA-MB-453 (MTT, IC50=0.18; Cell counting, IC50=0.19), MDA-MB-468 (MTT, IC50=0.15; Cell counting, IC50=0.17)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U937 cells, HL-60 cells, NB4 cells, KBM5 cells, K562 cells, Jurkat cells
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Concentration:0.039 μM, 0.078 μM, 0.16 μM, 0.3 μM, 0.6 μM
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Incubation Time:48 hours
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Result:Inhibited all the tested cell lines.
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Cell Line:NB4 cells, K562 cells, Jurkat cells
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Concentration:0.039 μM, 0.078 μM, 0.16 μM, 0.3 μM, 0.6 μM
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Incubation Time:48 hours
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Result:Inhibited the phosphorylation of AurA Thr288 (p-AurA).
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Cell Line:K562, K562/G, 32D-p210 and 32D-T315I cells
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Concentration:0.3 μM, 0.6 μM
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Incubation Time:48 hours
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Result:Induced polyploidization in the tested cells.
AKI603 exhibits moderate oral bioavailability (rat 28.7%) and Cmax (rat 202.4 μg/L) following oral administration (rat 25 mg/kg)[3].
AKI603 exhibits terminal elimination half-life (rat 8.9 h) following intravenous administration (rat 2.5 mg/kg)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c nude mice, with KBM5-T315I cells xenografted[1]
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Dosage:12.5 mg/kg, 25 mg/kg
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Administration:Intraperitoneal injection, every 2 days, for 14 days
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Result:Significantly inhibited the growth of tumors.
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Animal Model:SD rats (220-280 g)[3]
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Dosage:2.5 mg/kg for i.v.; 25 mg/kg for p.o. (Pharmacokinetic Analysis)
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Administration:Intravenous injection, oral administration
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Result:Oral bioavailability (28.7%), Cmax (202.4 μg/L), T1/2 (8.9 h)
Chemical Information
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No. CAS 1432515-73-5
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Appearance Solid
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Peso molecular 409.45
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Fòrmula C19H23N9O2
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Color White to yellow
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SMILES
O=[N+]([O-])C1=CC=C(C=C1)NC2=NC(N3CCN(CC3)C)=CC(NC4=NNC(C)=C4)=N2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 125 mg/mL (305.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 6.25 mg/mL (15.26 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 6.25 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 (62.5 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (279 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Le-Xun Wang, et al. Aurora A Kinase Inhibitor AKI603 Induces Cellular Senescence in Chronic Myeloid Leukemia Cells Harboring T315I Mutation. Sci Rep. 2016 Nov 8;6:35533. [Content Brief]
[2]. Fei-Meng Zheng, et al. A novel small molecule aurora kinase inhibitor attenuates breast tumor-initiating cells and overcomes drug resistance. Mol Cancer Ther. 2014 Aug;13(8):1991-2003. [Content Brief]
[3]. Zhenzhen Zhao, et al. Determination of a novel Aurora-A (AurA) kinase AKI603 by UPLC-MS/MS and its application to a bioavailability study in rat. J Pharm Biomed Anal. 2016 Jun 5;125:303-9. [Content Brief]
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, 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 | 2.4423 mL | 12.2115 mL | 24.4230 mL | 61.0575 mL |
| 5 mM | 0.4885 mL | 2.4423 mL | 4.8846 mL | 12.2115 mL | |
| 10 mM | 0.2442 mL | 1.2212 mL | 2.4423 mL | 6.1058 mL | |
| 15 mM | 0.1628 mL | 0.8141 mL | 1.6282 mL | 4.0705 mL | |
| 20 mM | 0.1221 mL | 0.6106 mL | 1.2212 mL | 3.0529 mL | |
| 25 mM | 0.0977 mL | 0.4885 mL | 0.9769 mL | 2.4423 mL | |
| 30 mM | 0.0814 mL | 0.4071 mL | 0.8141 mL | 2.0353 mL | |
| 40 mM | 0.0611 mL | 0.3053 mL | 0.6106 mL | 1.5264 mL | |
| 50 mM | 0.0488 mL | 0.2442 mL | 0.4885 mL | 1.2212 mL | |
| 60 mM | 0.0407 mL | 0.2035 mL | 0.4071 mL | 1.0176 mL | |
| 80 mM | 0.0305 mL | 0.1526 mL | 0.3053 mL | 0.7632 mL | |
| 100 mM | 0.0244 mL | 0.1221 mL | 0.2442 mL | 0.6106 mL |
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